VEGFA

Summary

VEGFA (vascular endothelial growth factor A, HGNC:12680) is a protein-coding gene on chromosome 6p21.1, encoding Vascular endothelial growth factor A, long form (P15692). Participates in the induction of key genes involved in the response to hypoxia and in the induction of angiogenesis such as HIF1A. In precision oncology, VEGFA Decreased Peri-therapeutic Expression confers sensitivity to Levoleucovorin + Irinotecan + Bevacizumab + Fluorouracil in Colorectal Cancer (CIViC Level B).

This gene is a member of the PDGF/VEGF growth factor family. It encodes a heparin-binding protein, which exists as a disulfide-linked homodimer. This growth factor induces proliferation and migration of vascular endothelial cells, and is essential for both physiological and pathological angiogenesis. Disruption of this gene in mice resulted in abnormal embryonic blood vessel formation. This gene is upregulated in many known tumors and its expression is correlated with tumor stage and progression. Elevated levels of this protein are found in patients with POEMS syndrome, also known as Crow-Fukase syndrome. Allelic variants of this gene have been associated with microvascular complications of diabetes 1 (MVCD1) and atherosclerosis. Alternatively spliced transcript variants encoding different isoforms have been described. There is also evidence for alternative translation initiation from upstream non-AUG (CUG) codons resulting in additional isoforms. A recent study showed that a C-terminally extended isoform is produced by use of an alternative in-frame translation termination codon via a stop codon readthrough mechanism, and that this isoform is antiangiogenic. Expression of some isoforms derived from the AUG start codon is regulated by a small upstream open reading frame, which is located within an internal ribosome entry site. The levels of VEGF are increased during infection with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), thus promoting inflammation by facilitating recruitment of inflammatory cells, and by increasing the level of angiopoietin II (Ang II), one of two products of the SARS-CoV-2 binding target, angiotensin-converting enzyme 2 (ACE2). In turn, Ang II facilitates the elevation of VEGF, thus forming a vicious cycle in the release of inflammatory cytokines.

Source: NCBI Gene 7422 — RefSeq curated summary.

At a glance

• Gene–disease (curated): congenital heart disease (Limited, ClinGen)
• GWAS associations: 260
• Clinical variants (ClinVar): 109 total — 2 likely-pathogenic
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 1 curated variant–drug association
• Dosage sensitivity (ClinGen): haploinsufficiency little evidence, triplosensitivity no evidence
• MANE Select transcript: NM_003376

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:12680
Approved symbol	VEGFA
Name	vascular endothelial growth factor A
Location	6p21.1
Locus type	gene with protein product
Status	Approved
Aliases	VEGF-A, VPF
Ensembl gene	ENSG00000112715
Ensembl biotype	protein_coding
OMIM	192240
Entrez	7422

Gene structure

Transcript identifiers

Ensembl transcripts: 26 — 20 protein_coding, 6 retained_intron

ENST00000230480, ENST00000324450, ENST00000372055, ENST00000372064, ENST00000372067, ENST00000372077, ENST00000413642, ENST00000417285, ENST00000425836, ENST00000457104, ENST00000476772, ENST00000480614, ENST00000482630, ENST00000493786, ENST00000497139, ENST00000512683, ENST00000518538, ENST00000518689, ENST00000518824, ENST00000519767, ENST00000520265, ENST00000520948, ENST00000523125, ENST00000523873, ENST00000523950, ENST00000672860

RefSeq mRNA: 20 — MANE Select: NM_003376 NM_001025366, NM_001025367, NM_001025368, NM_001025369, NM_001025370, NM_001033756, NM_001171622, NM_001171623, NM_001171624, NM_001171625, NM_001171626, NM_001171627, NM_001171628, NM_001171629, NM_001171630, NM_001204384, NM_001204385, NM_001287044, NM_001317010, NM_003376

CCDS: CCDS34457, CCDS34458, CCDS47432, CCDS47433, CCDS47434, CCDS47435, CCDS4907, CCDS55007, CCDS55008, CCDS55009, CCDS55010, CCDS55011, CCDS55012, CCDS55013, CCDS55014, CCDS55015, CCDS69125

Canonical transcript exons

ENST00000672860 — 8 exons

Exon	Start	End
ENSE00000753776	43780732	43780803
ENSE00001431654	43784541	43786487
ENSE00003501088	43778460	43778536
ENSE00003595535	43777469	43777665
ENSE00003605110	43778889	43778918
ENSE00003650262	43781956	43782087
ENSE00003650678	43774341	43774392
ENSE00003931448	43770211	43771312

Expression profiles

Bgee: expression breadth ubiquitous, 297 present calls, max score 99.59.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 73.5852 / max 3079.2377, expressed in 1747 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
67927	66.8995	1714
67928	4.5180	1406
67929	1.2051	636
67934	0.6730	367
67932	0.1364	44
67931	0.1343	42
67930	0.0189	8

Top tissues by expression

298 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
right lobe of thyroid gland	UBERON:0001119	99.59	gold quality
left lobe of thyroid gland	UBERON:0001120	99.53	gold quality
thyroid gland	UBERON:0002046	99.51	gold quality
renal glomerulus	UBERON:0000074	99.25	gold quality
metanephric glomerulus	UBERON:0004736	99.17	gold quality
pigmented layer of retina	UBERON:0001782	99.12	gold quality
retina	UBERON:0000966	99.10	gold quality
cartilage tissue	UBERON:0002418	98.92	gold quality
right lobe of liver	UBERON:0001114	98.89	gold quality
apex of heart	UBERON:0002098	98.88	gold quality
pericardium	UBERON:0002407	98.79	gold quality
right atrium auricular region	UBERON:0006631	98.61	gold quality
ventricular zone	UBERON:0003053	98.58	gold quality
cardiac atrium	UBERON:0002081	98.55	gold quality
gall bladder	UBERON:0002110	98.54	gold quality
gastrocnemius	UBERON:0001388	98.51	gold quality
metanephros	UBERON:0000081	98.49	gold quality
body of uterus	UBERON:0009853	98.44	gold quality
lower esophagus mucosa	UBERON:0035834	98.44	gold quality
mucosa of paranasal sinus	UBERON:0005030	98.41	gold quality
body of tongue	UBERON:0011876	98.40	gold quality
islet of Langerhans	UBERON:0000006	98.38	gold quality
vena cava	UBERON:0004087	98.37	gold quality
cortex of kidney	UBERON:0001225	98.34	gold quality
type B pancreatic cell	CL:0000169	98.33	gold quality
renal medulla	UBERON:0000362	98.33	gold quality
omental fat pad	UBERON:0010414	98.32	gold quality
peritoneum	UBERON:0002358	98.31	gold quality
saphenous vein	UBERON:0007318	98.29	gold quality
adipose tissue of abdominal region	UBERON:0007808	98.23	gold quality

Single-cell (SCXA)

Detected in 11 experiment(s), a significant marker in 8.

Experiment	Marker?	Max mean expression
E-MTAB-10662	yes	2577.09
E-MTAB-9435	yes	939.73
E-GEOD-84465	yes	654.13
E-MTAB-8410	yes	346.82
E-CURD-119	yes	31.46
E-HCAD-10	yes	18.31
E-GEOD-130148	yes	6.40
E-GEOD-86618	no	174.76
E-ENAD-17	no	90.57
E-ENAD-27	no	11.14
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

9 targets.

Target	Regulation
BCL2	Activation
DLL4	Activation
EFNB2	Activation
HES1	Activation
NOTCH1	Activation
NOTCH4	Activation
NR2F2	Repression
RGCC	Activation
TGFB2	Repression

Upstream regulators (CollecTRI, top): ADM2, AHR, AP1, AR, ARNT, ATF3, ATF4, ATF6, ATM, BHLHE40, BHLHE41, BMAL1, BRCA1, CEBPA, COPS5, CREB1, CTCF, CTNNB1, DDIT3, DLX4, DNAJC1, DNMT1, DNMT3A, E2F1, E2F3, E2F7, E2F8, EGR1, ELK3, EP300, EPAS1, ESR1, ESR2, ESRRA, ETS1, ETV4, ETV6, FHL1, FOS, FOXC1

miRNA regulators (miRDB)

165 targeting VEGFA, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-6748-5P	100.00	65.81	1057
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-5193	100.00	67.26	1744
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-495-3P	99.96	72.81	4197

Functional genomics

ClinGen dosage: haploinsufficiency 1 (little evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

• Includes data regarding non-AUG translation initiation (CUG) of VEGF (PMID:11352659)
• Includes data regarding non-AUG translation initiation (CUG) of VEGF (PMID:11563986)
• upregulated in eye in experimental herpesvirus retinopathy (PMID:11642726)
• Thrombin induces increased expression and secretion of VEGF from human FS4 fibroblasts, DU145 prostate cells and CHRF megakaryocytes. (PMID:11686329)
• The VEGF levels were significantly higher in recurrent ALL compared with newly diagnosed ALL. (PMID:11705851)
• VEGF levels were elevated in patients with invasive cancer of ductal/no specific type, ductal carcinoma in situ, and estrogen receptor (ER)-positive tumors. (PMID:11705867)
• Includes data regarding non-AUG translation initiation (CUG) of VEGF (PMID:11731620)
• induction in human glioblastoma cells by acidic extracellular pH via ERK1/2 MAPK signaling pathway (PMID:11741977)
• Significant association with poor survival by VEGF. (PMID:11742492)
• Vascular endothelial growth factor expression in serous ovarian carcinoma: relationship with high mitotic activity and high FIGO stage. (PMID:11748975)
• both VEGF-induced PI 3-kinase activation and beta(1) integrin-mediated binding to fibronectin are required for the recruitment and activation of PKC alpha. (PMID:11751905)
• VEGF expression and intratumoral microvessel density (IMVD) can be considered as a biological indicator of malignant potential in brain astrocytoma. (PMID:11783119)
• Vascular endothelial growth factor modulates neutrophil transendothelial migration via up-regulation of interleukin-8 in human brain microvascular endothelial cells (PMID:11784713)
• modulation of signaling and angiogenic effects by PTEN (PMID:11784722)
• upregulation by interleukin-1 beta in vascular smooth muscle cells via the P38 mitogen-activated protein kinase pathway (PMID:11806247)
• Vascular endothelial growth factor-A(165) induces progression of melanoma brain metastases without induction of sprouting angiogenesis. (PMID:11809675)
• Up-regulation of vascular endothelial growth factor by membrane-type 1 matrix metalloproteinase stimulates human glioma xenograft growth and angiogenesis. (PMID:11809713)
• essential for developmental angiogenesis and is also required for female reproductive functions and endochondral bone formation. (PMID:11815711)
• VEGF plays an important role in the oncogenesis of human gastric cancer. (PMID:11819817)
• Platelets and vascular endothelial growth factor (VEGF): a morphological and functional study. (PMID:11824377)
• VEGF is highly related to PVBE and angiogenesis of meningoma. (PMID:11831981)
• bFGF and VEGF were synergistic in terms of DAF expression, resulting in enhanced endothelial cytoprotection (PMID:11832343)
• A 40-bp RNA element that mediates stabilization of vascular endothelial growth factor mRNA by HuR. (PMID:11834731)
• Plasma vascular endothelial growth factor is useful in assessing progression of breast cancer post surgery and during adjuvant treatment. (PMID:11836562)
• VEGF and flt-1 are upregulated in blood vessels in many organs of acute Kawasaki Disease (PMID:11839635)
• Blood levels are elevated in myelodysplastic syndromes and in acute myeloid leukemia. VEGF corrected for the peripheral blood platelet count is a marker of disease progression in MDS. (PMID:11847008)
• NMR structure of a phage-derived peptide antagonist in complex with vascular endothelial growth factor (PMID:11866530)
• Vascular endothelial growth factor modulates the Tie-2:Tie-1 receptor complex (PMID:11866538)
• free plasma VEGF levels are high in chronic renal impairment; may contribute to the endothelial dysfunction of uraemia (PMID:11867956)
• prognostic value of matched preoperative serum and plasma vascular endothelial growth factor concentrations in patients with colorectal cancer. (PMID:11875709)
• Prognostic significance of VEGF expression in bone marrow cells in chronic phase chronic myeloid leukemia. (PMID:11877311)
• VEGF upregulates BCL-2 expression and is associated with decreased apoptosis in neuroblastoma cells. (PMID:11877669)
• Chemoattractive and proliferative effects of VEGF-A have been demonstrated on primary human osteoblasts. (PMID:11882460)
• Plasma VEGF levels are significantly increased in chronic myeloproliferative disorders. The highest levles were found in CMD with essential thrombocythemia. Levels were significantly higher in CMD patients with vascular complications. (PMID:11891801)
• VEGF may act as a growth factor for both endothelial cells and tumor cells. (PMID:11908876)
• Activation of vascular endothelial growth factor A transcription in tumorigenic glioblastoma cell lines by an enhancer with cell type-specific DNase I accessibility (PMID:11912213)
• overexpression in mesangial cells by advanced glycation end products (PMID:11912219)
• tumor cell-VEGF induction may promote angiogenesis in adenocarcinoma of the lung; tumor cell expression may be important prognostic factor in adenocarcinoma of the lung (PMID:11920479)
• expression of tissue factor (TF) and VEGF is frequently observed in colorectal cancer and TF expression is significantly related with VEGF expression and microvessel density (PMID:11921018)
• VEGF as a mediator of OHSS. (PMID:11930687)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	vegfab	ENSDARG00000034700
danio_rerio	vegfaa	ENSDARG00000103542
mus_musculus	Vegfa	ENSMUSG00000023951
rattus_norvegicus	Vegfa	ENSRNOG00000019598

Paralogs (4): PGF (ENSG00000119630), VEGFC (ENSG00000150630), VEGFD (ENSG00000165197), VEGFB (ENSG00000173511)

Protein

Protein identifiers

Vascular endothelial growth factor A, long form — P15692 (reviewed: P15692)

Alternative names: Vascular permeability factor

All UniProt accessions (14): P15692, A0A0A0MR43, A0A0A0MRQ4, A0A0A0MSH5, A0A0A0MSH7, A0A0A0MSI7, A0A0A0MTB2, A0A0Y0IMM4, A0A5F9ZH41, A2A2V4, H0YBI8, H0YBZ0, H3BLW8, J3KPA4

UniProt curated annotations — full annotation on UniProt →

Function. Participates in the induction of key genes involved in the response to hypoxia and in the induction of angiogenesis such as HIF1A. Involved in protecting cells from hypoxia-mediated cell death. Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. Binds to the NRP1/neuropilin-1 receptor. Binding to NRP1 initiates a signaling pathway needed for motor neuron axon guidance and cell body migration, including for the caudal migration of facial motor neurons from rhombomere 4 to rhombomere 6 during embryonic development. Also binds the DEAR/FBXW7-AS1 receptor. Binds to the KDR receptor but does not activate downstream signaling pathways, does not activate angiogenesis and inhibits tumor growth.

Subunit / interactions. Homodimer; disulfide-linked. Also found as heterodimer with PGF. Interacts with NRP1. Interacts with isoform 2 of BSG. Interacts with CD82; this interaction inhibits VEGFA-mediated signaling pathway.

Subcellular location. Cytoplasm. Nucleus Secreted Endoplasmic reticulum. Golgi apparatus. Secreted. Extracellular space. Extracellular matrix Secreted Secreted Secreted.

Tissue specificity. Higher expression in pituitary tumors than the pituitary gland. Widely expressed. Widely expressed. Widely expressed. Not widely expressed. Not widely expressed.

Post-translational modifications. Produced by use of an alternative upstream CUG codon and post-translationally processed into the N-terminal N-VEGF form and the C-terminal secreted VEGFA form.

Disease relevance. Microvascular complications of diabetes 1 (MVCD1) [MIM:603933] Pathological conditions that develop in numerous tissues and organs as a consequence of diabetes mellitus. They include diabetic retinopathy, diabetic nephropathy leading to end-stage renal disease, and diabetic neuropathy. Diabetic retinopathy remains the major cause of new-onset blindness among diabetic adults. It is characterized by vascular permeability and increased tissue ischemia and angiogenesis. Disease susceptibility is associated with variants affecting the gene represented in this entry.

Induction. By hypoxia. Regulated by growth factors, cytokines, gonadotropins, nitric oxide, hypoglycemia and oncogenic mutations.

Miscellaneous. Produced by alternative promoter usage and alternative initiation. Starts at an alternative upstream CUG codon. Produced by alternative promoter usage and alternative initiation. Starts at an alternative upstream CUG codon. Produced by alternative promoter usage and alternative initiation. Starts at an alternative upstream CUG codon. Produced by alternative promoter usage and alternative initiation. Starts at an alternative upstream CUG codon. Starts at an alternative upstream CUG codon. Starts at an alternative upstream CUG codon. Starts at an alternative upstream CUG codon. Starts at an alternative upstream CUG codon.

Similarity. Belongs to the PDGF/VEGF growth factor family.

Isoforms (17)

UniProt ID	Names	Canonical?
P15692-13	L-VEGF189	yes
P15692-1	VEGF206
P15692-2	VEGF189
P15692-3	VEGF183
P15692-4	VEGF165, VEGF
P15692-5	VEGF148
P15692-6	VEGF145
P15692-8	VEGF165B
P15692-9	VEGF121
P15692-10	VEGF111
P15692-11	L-VEGF165
P15692-12	L-VEGF121
P15692-14	L-VEGF206
P15692-15	15
P15692-16	16
P15692-17	17
P15692-18	18

RefSeq proteins (20): NP_001020537, NP_001020538, NP_001020539, NP_001020540, NP_001020541, NP_001028928, NP_001165093, NP_001165094, NP_001165095, NP_001165096, NP_001165097, NP_001165098, NP_001165099, NP_001165100, NP_001165101, NP_001191313, NP_001191314, NP_001273973, NP_001303939, NP_003367* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000072	PDGF/VEGF_dom	Domain
IPR023581	PD_growth_factor_CS	Conserved_site
IPR027928	VEGF_C	Domain
IPR029034	Cystine-knot_cytokine	Homologous_superfamily
IPR036841	VEGF_C_sf	Homologous_superfamily
IPR050507	PDGF/VEGF_growth_factor	Family

Pfam: PF00341, PF14554

UniProt features (50 total): splice variant 13, strand 9, compositionally biased region 6, disulfide bond 5, helix 4, turn 4, chain 3, region of interest 3, sequence conflict 2, glycosylation site 1

Structure

Experimental structures (PDB)

56 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
1MKK	X-RAY DIFFRACTION	1.32
9JU1	X-RAY DIFFRACTION	1.45
9KKU	X-RAY DIFFRACTION	1.46
4GLN	X-RAY DIFFRACTION	1.6
4GLS	X-RAY DIFFRACTION	1.6
6ZBR	X-RAY DIFFRACTION	1.6
6ZFL	X-RAY DIFFRACTION	1.6
1FLT	X-RAY DIFFRACTION	1.7
4KZN	X-RAY DIFFRACTION	1.71
4QAF	X-RAY DIFFRACTION	1.8
6Z13	X-RAY DIFFRACTION	1.8
6ZCD	X-RAY DIFFRACTION	1.8
3QTK	X-RAY DIFFRACTION	1.85
1VPP	X-RAY DIFFRACTION	1.9
2VPF	X-RAY DIFFRACTION	1.93
5DN2	X-RAY DIFFRACTION	1.95
1MJV	X-RAY DIFFRACTION	2.1
5HHC	X-RAY DIFFRACTION	2.1
5HHD	X-RAY DIFFRACTION	2.1
6Z3F	X-RAY DIFFRACTION	2.1
5O4E	X-RAY DIFFRACTION	2.15
7KEZ	X-RAY DIFFRACTION	2.31
7LL8	X-RAY DIFFRACTION	2.31
7KF0	X-RAY DIFFRACTION	2.32
1BJ1	X-RAY DIFFRACTION	2.4
1CZ8	X-RAY DIFFRACTION	2.4
3P9W	X-RAY DIFFRACTION	2.41
7KF1	X-RAY DIFFRACTION	2.45
1MKG	X-RAY DIFFRACTION	2.5
1VPF	X-RAY DIFFRACTION	2.5

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P15692-F1	65.32	0.29

Antibody-complex structures (SAbDab): 18 — 1BJ1, 1CZ8, 1TZH, 1TZI, 2FJG, 2FJH, 2QR0, 3BDY, 3P9W, 4ZFF, 5FV1, 5FV2, 6BFT, 6T9D, 7KEZ, 7KF0, 7KF1, 8UWZ

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Disulfide bonds (5): 232–274, 257, 263–308, 266, 267–310

Glycosylation sites (1): 281

Function

Pathways and Gene Ontology

Reactome pathways

10 pathways

ID	Pathway
R-HSA-114608	Platelet degranulation
R-HSA-1234158	Regulation of gene expression by Hypoxia-inducible Factor
R-HSA-194138	Signaling by VEGF
R-HSA-194313	VEGF ligand-receptor interactions
R-HSA-195399	VEGF binds to VEGFR leading to receptor dimerization
R-HSA-6785807	Interleukin-4 and Interleukin-13 signaling
R-HSA-8866910	TFAP2 (AP-2) family regulates transcription of growth factors and their receptors
R-HSA-4420097	VEGFA-VEGFR2 Pathway
R-HSA-5218921	VEGFR2 mediated cell proliferation
R-HSA-9679191	Potential therapeutics for SARS

MSigDB gene sets: 1080 (showing top): PID_SHP2_PATHWAY, GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_PLATELET_DERIVED_GROWTH_FACTOR_RECEPTOR_SIGNALING_PATHWAY, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_ENDOTHELIAL_CELL_DEVELOPMENT, TGGTGCT_MIR29A_MIR29B_MIR29C, RNGTGGGC_UNKNOWN, VERHAAK_AML_WITH_NPM1_MUTATED_DN, FXR_IR1_Q6, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, GOBP_HEMATOPOIETIC_PROGENITOR_CELL_DIFFERENTIATION, MODULE_52, GOBP_POSITIVE_REGULATION_OF_REPRODUCTIVE_PROCESS, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYONIC_HEMOPOIESIS

GO Biological Process (130): negative regulation of transcription by RNA polymerase II (GO:0000122), angiogenesis (GO:0001525), ovarian follicle development (GO:0001541), branching involved in blood vessel morphogenesis (GO:0001569), vasculogenesis (GO:0001570), response to hypoxia (GO:0001666), in utero embryonic development (GO:0001701), kidney development (GO:0001822), positive regulation of protein phosphorylation (GO:0001934), endothelial cell proliferation (GO:0001935), positive regulation of endothelial cell proliferation (GO:0001938), lymphangiogenesis (GO:0001946), sprouting angiogenesis (GO:0002040), cell migration involved in sprouting angiogenesis (GO:0002042), positive regulation of neuroblast proliferation (GO:0002052), epithelial cell maturation (GO:0002070), positive regulation of receptor internalization (GO:0002092), basophil chemotaxis (GO:0002575), positive regulation of leukocyte migration (GO:0002687), heart morphogenesis (GO:0003007), outflow tract morphogenesis (GO:0003151), coronary vein morphogenesis (GO:0003169), regulation of transcription by RNA polymerase II (GO:0006357), apoptotic process (GO:0006915), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), nervous system development (GO:0007399), neuroblast proliferation (GO:0007405), mesoderm development (GO:0007498), lactation (GO:0007595), positive regulation of cell population proliferation (GO:0008284), regulation of cell shape (GO:0008360), positive regulation of endothelial cell migration (GO:0010595), positive regulation of gene expression (GO:0010628), negative regulation of gene expression (GO:0010629), negative regulation of epithelial to mesenchymal transition (GO:0010719), obsolete regulation of nitric oxide mediated signal transduction (GO:0010749), monocyte differentiation (GO:0030224), macrophage differentiation (GO:0030225), lung development (GO:0030324), positive regulation of cell migration (GO:0030335)

GO Molecular Function (16): fibronectin binding (GO:0001968), cytokine activity (GO:0005125), platelet-derived growth factor receptor binding (GO:0005161), vascular endothelial growth factor receptor binding (GO:0005172), growth factor activity (GO:0008083), heparin binding (GO:0008201), transmembrane receptor protein tyrosine kinase activator activity (GO:0030297), neuropilin binding (GO:0038191), chemoattractant activity (GO:0042056), identical protein binding (GO:0042802), protein homodimerization activity (GO:0042803), vascular endothelial growth factor receptor 1 binding (GO:0043183), vascular endothelial growth factor receptor 2 binding (GO:0043184), receptor ligand activity (GO:0048018), extracellular matrix binding (GO:0050840), protein binding (GO:0005515)

GO Cellular Component (13): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), nucleus (GO:0005634), cytoplasm (GO:0005737), endoplasmic reticulum (GO:0005783), Golgi apparatus (GO:0005794), adherens junction (GO:0005912), cell surface (GO:0009986), membrane (GO:0016020), secretory granule (GO:0030141), extracellular matrix (GO:0031012), platelet alpha granule lumen (GO:0031093), VEGF-A complex (GO:1990150)

Reactome top-level categories

Rollup of top-9 pathways:

Category	Pathways
Signaling by VEGF	2
Response to elevated platelet cytosolic Ca2+	1
Cellular response to hypoxia	1
Signaling by Receptor Tyrosine Kinases	1
VEGF ligand-receptor interactions	1
Signaling by Interleukins	1
Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors	1
VEGFA-VEGFR2 Pathway	1
SARS-CoV Infections	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
blood vessel morphogenesis	3
receptor ligand activity	3
intracellular membrane-bounded organelle	3
endomembrane system	3
anatomical structure formation involved in morphogenesis	2
angiogenesis	2
protein binding	2
growth factor receptor binding	2
signaling receptor activator activity	2
signaling receptor binding	2
vascular endothelial growth factor receptor binding	2
binding	2
cytoplasm	2
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
female gonad development	1
anatomical structure development	1
branching morphogenesis of an epithelial tube	1
cell differentiation	1
response to stress	1
response to decreased oxygen levels	1
chordate embryonic development	1
animal organ development	1
renal system development	1
regulation of protein phosphorylation	1
protein phosphorylation	1
positive regulation of protein modification process	1
positive regulation of phosphorylation	1
epithelial cell proliferation	1
endothelial cell proliferation	1
regulation of endothelial cell proliferation	1
positive regulation of epithelial cell proliferation	1
anatomical structure morphogenesis	1
lymph vessel morphogenesis	1
sprouting angiogenesis	1
blood vessel endothelial cell migration	1
neuroblast proliferation	1
positive regulation of neurogenesis	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

53 interactions, top by confidence:

A	B	Type	Score
VEGFA	FLT1	psi-mi:“MI:0407”(direct interaction)	0.820
FLT1	VEGFA	psi-mi:“MI:0407”(direct interaction)	0.820
VEGFA	FLT1	psi-mi:“MI:0915”(physical association)	0.820
FLT1	VEGFA	psi-mi:“MI:0915”(physical association)	0.820
VEGFA	KDR	psi-mi:“MI:0407”(direct interaction)	0.810
VEGFA	KDR	psi-mi:“MI:0915”(physical association)	0.810
KDR	VEGFA	psi-mi:“MI:2364”(proximity)	0.810
NRP1	VEGFA	psi-mi:“MI:0915”(physical association)	0.770
VEGFA	NRP1	psi-mi:“MI:0915”(physical association)	0.770
VEGFA	VEGFA	psi-mi:“MI:0407”(direct interaction)	0.720
KDR	GREM1	psi-mi:“MI:0915”(physical association)	0.640
VEGFB	VEGFA	psi-mi:“MI:0914”(association)	0.480
VEGFB	VEGFA	psi-mi:“MI:2364”(proximity)	0.480
Nrp1	VEGFA	psi-mi:“MI:0407”(direct interaction)	0.440
VEGFA	THBS1	psi-mi:“MI:0915”(physical association)	0.400
U2AF1	VEGFA	psi-mi:“MI:0915”(physical association)	0.370

BioGRID (114): VEGFA (Affinity Capture-MS), VEGFA (Affinity Capture-RNA), VEGFA (Affinity Capture-RNA), VEGFA (Protein-RNA), VEGFA (Co-localization), VEGFA (Co-localization), VEGFA (Two-hybrid), KDR (Co-localization), PTPRB (Affinity Capture-Western), PTPRZ1 (Affinity Capture-Western), VEGFA (Affinity Capture-Western), VEGFA (Affinity Capture-Western), VEGFA (Co-localization), VEGFA (Co-localization), VEGFA (Affinity Capture-Western)

ESM2 similar proteins: A4D1S0, A4K2S4, A6NMD0, B9A064, F8WCM5, H7C350, O00220, O14931, O15533, O70146, O73895, O75298, O76081, P01854, P01883, P14138, P15692, P15814, P16382, P20764, P24394, P49763, P61484, P83743, Q00731, Q0VCS0, Q15569, Q3UM83, Q5R8H1, Q5RFR2, Q5TJE4, Q63257, Q63572, Q68D85, Q6P050, Q6PZD2, Q6WG24, Q7TQM3, Q863Z5, Q8MJ02

Diamond homologs: B0VXV3, B0VXV4, C0HM96, C0K3N1, C0K3N2, C0K3N3, C0K3N4, C0K3N5, O35251, O35485, O35757, O43915, O73682, P0DL42, P0DW97, P0DW98, P15691, P15692, P16612, P26617, P49151, P49763, P49764, P49765, P49766, P49767, P50412, P52584, P52585, P67860, P67861, P67862, P67863, P67964, P67965, P82475, P83906, P83942, P97946, P97953

SIGNOR signaling

18 interactions.

A	Effect	B	Mechanism
VEGFA	up-regulates	FLT1	binding
VEGFA	up-regulates	KDR	binding
VEGFA	“up-regulates quantity by expression”	DLL4	“transcriptional regulation”
HIC1	“down-regulates quantity by repression”	VEGFA	“transcriptional regulation”
RUNX2	“up-regulates quantity by expression”	VEGFA	“transcriptional regulation”
HIF1A	“up-regulates quantity”	VEGFA	“transcriptional regulation”
VEGFA	up-regulates	Angiogenesis
Aflibercept	“down-regulates activity”	VEGFA	“chemical inhibition”
STAT3	“up-regulates quantity by expression”	VEGFA	“transcriptional regulation”
bevacizumab	“down-regulates activity”	VEGFA	binding
ZMYND8	“down-regulates quantity by repression”	VEGFA	“transcriptional regulation”
hsa-miR-30a-3p	“down-regulates quantity by repression”	VEGFA	“post transcriptional regulation”
hsa-miR-199a-5p	“down-regulates quantity by repression”	VEGFA	“post transcriptional regulation”
hsa-miR-200b-5p	“down-regulates quantity by repression”	VEGFA	“post transcriptional regulation”
MYOD/E12E47	“up-regulates quantity by expression”	VEGFA	“transcriptional regulation”
MYOD1	“up-regulates quantity by expression”	VEGFA	“transcriptional regulation”
MYC	“up-regulates quantity by expression”	VEGFA	“transcriptional regulation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 23 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

GO biological processes:

GO term	Partners	Fold	FDR
sprouting angiogenesis	5	114.6×	2e-07
vascular endothelial growth factor receptor signaling pathway	5	114.6×	2e-07
positive regulation of angiogenesis	5	27.5×	8e-05
positive regulation of ERK1 and ERK2 cascade	6	24.3×	2e-05
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	6	22.4×	2e-05
positive regulation of cell migration	5	14.7×	8e-04
negative regulation of apoptotic process	6	9.9×	8e-04

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

109 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	2
Uncertain significance	61
Likely benign	18
Benign	8

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
2632972	NM_003376.6(VEGFA):c.576_589del (p.Ala193fs)	Likely pathogenic
809941	NM_003376.6(VEGFA):c.19_22dup (p.Thr8fs)	Likely pathogenic

SpliceAI

1191 predictions. Top by Δscore:

Variant	Effect	Δscore
6:43777464:T:G	acceptor_gain	1.0000
6:43777464:T:TA	acceptor_gain	1.0000
6:43777464:TGCA:T	acceptor_loss	1.0000
6:43777467:A:AG	acceptor_gain	1.0000
6:43777467:AGT:A	acceptor_gain	1.0000
6:43777467:AGTG:A	acceptor_gain	1.0000
6:43777468:G:GA	acceptor_gain	1.0000
6:43777468:GT:G	acceptor_gain	1.0000
6:43777468:GTG:G	acceptor_gain	1.0000
6:43777468:GTGG:G	acceptor_gain	1.0000
6:43777468:GTGGT:G	acceptor_gain	1.0000
6:43777662:GCAG:G	donor_gain	1.0000
6:43777664:AGGT:A	donor_loss	1.0000
6:43777666:GT:G	donor_loss	1.0000
6:43778455:TCCA:T	acceptor_loss	1.0000
6:43778458:A:AG	acceptor_gain	1.0000
6:43778458:A:AT	acceptor_loss	1.0000
6:43778459:G:GC	acceptor_gain	1.0000
6:43778459:GA:G	acceptor_gain	1.0000
6:43778459:GAT:G	acceptor_gain	1.0000
6:43778459:GATT:G	acceptor_gain	1.0000
6:43778459:GATTA:G	acceptor_gain	1.0000
6:43778533:GCAG:G	donor_gain	1.0000
6:43778534:CAGG:C	donor_loss	1.0000
6:43778535:AG:A	donor_loss	1.0000
6:43778536:GG:G	donor_loss	1.0000
6:43778537:G:A	donor_loss	1.0000
6:43778538:T:A	donor_loss	1.0000
6:43778878:A:AG	acceptor_gain	1.0000
6:43778914:GAAAA:G	donor_gain	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000200646 (6:43785229 C>T), RS1000308091 (6:43779980 G>A), RS1000758573 (6:43778679 T>C), RS1000935188 (6:43784086 A>G), RS1001230999 (6:43768209 A>G), RS1001732327 (6:43774816 C>T), RS1001797852 (6:43774338 C>T), RS1001830377 (6:43776480 A>C,G), RS1001852768 (6:43779237 T>C,G), RS1001905120 (6:43779458 G>A), RS1001985161 (6:43785712 C>G), RS1001991928 (6:43783019 C>T), RS1002016923 (6:43773417 C>T), RS1002078454 (6:43774594 A>G), RS1002178029 (6:43776805 A>C)

Disease associations

OMIM: gene MIM:192240 | disease phenotypes: MIM:603933, MIM:601518

GenCC curated gene-disease

Disease	Classification	Inheritance
congenital heart disease	Limited	Autosomal dominant

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
congenital heart disease	Limited	AD

Mondo (4): microvascular complications of diabetes, susceptibility to, 1 (MONDO:0011386), cholangiocarcinoma (MONDO:0019087), prostate cancer, hereditary, 1 (MONDO:0011098), congenital heart disease (MONDO:0005453)

Orphanet (2): Cholangiocarcinoma (Orphanet:70567), Familial prostate cancer (Orphanet:1331)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

260 associations (top):

Study	Trait	p-value
GCST000167_7	Type 2 diabetes	4.000000e-06
GCST000649_11	Chronic kidney disease	9.000000e-14
GCST000829_2	Waist-hip ratio	6.000000e-25
GCST001100_4	Age-related macular degeneration	9.000000e-09
GCST001155_4	Vascular endothelial growth factor levels	2.000000e-26
GCST001401_1	Coronary heart disease	7.000000e-08
GCST001465_9	Adiponectin levels	3.000000e-08
GCST001791_17	Urate levels	8.000000e-16
GCST001856_32	Thyroid hormone levels	7.000000e-16
GCST001856_33	Thyroid hormone levels	2.000000e-10
GCST001856_52	Thyroid hormone levels	6.000000e-12
GCST001856_53	Thyroid hormone levels	5.000000e-06
GCST001856_54	Thyroid hormone levels	3.000000e-07
GCST001884_2	Age-related macular degeneration	9.000000e-16
GCST002063_2	Sexual dimorphism in anthropometric traits	2.000000e-11
GCST002216_9	Triglycerides	3.000000e-15
GCST002223_63	HDL cholesterol	2.000000e-11
GCST002352_27	Type 2 diabetes	2.000000e-07
GCST002782_141	Waist-to-hip ratio adjusted for body mass index	1.000000e-06
GCST002782_142	Waist-to-hip ratio adjusted for body mass index	2.000000e-06
GCST002782_217	Waist-to-hip ratio adjusted for body mass index	4.000000e-34
GCST002782_218	Waist-to-hip ratio adjusted for body mass index	3.000000e-27
GCST002782_219	Waist-to-hip ratio adjusted for body mass index	2.000000e-33
GCST002782_220	Waist-to-hip ratio adjusted for body mass index	1.000000e-26
GCST002782_73	Waist-to-hip ratio adjusted for body mass index	7.000000e-34
GCST002782_74	Waist-to-hip ratio adjusted for body mass index	1.000000e-29
GCST002782_75	Waist-to-hip ratio adjusted for body mass index	8.000000e-33
GCST002782_76	Waist-to-hip ratio adjusted for body mass index	1.000000e-28
GCST002783_259	Body mass index	3.000000e-06
GCST002783_388	Body mass index	9.000000e-07

EFO canonical traits (47, from GWAS)

EFO ID	Trait name
EFO:0004343	waist-hip ratio
EFO:0004502	adiponectin measurement
EFO:0004531	urate measurement
EFO:0004730	hormone measurement
EFO:0005951	sexual dimorphism
EFO:0004530	triglyceride measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0004340	body mass index
EFO:1001492	atrophic macular degeneration
EFO:0007789	BMI-adjusted waist circumference
EFO:0004753	interleukin 12 measurement
EFO:0008171	interleukin 13 measurement
EFO:0004750	interleukin 10 measurement
EFO:0008189	interleukin 7 measurement
EFO:0004318	smoking behavior
EFO:0008002	physical activity measurement
EFO:0004305	erythrocyte count
EFO:0004348	hematocrit
EFO:0007986	reticulocyte count
EFO:0004509	hemoglobin measurement
EFO:0008343	sex interaction measurement
EFO:0008007	age at assessment
EFO:0006336	diastolic blood pressure
EFO:0009270	heel bone mineral density
EFO:0004761	uric acid measurement
EFO:0009104	hyperuricemia
EFO:0009930	Calcium channel blocker use measurement
EFO:0009932	HMG CoA reductase inhibitor use measurement
EFO:0004329	alcohol drinking

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D018281	Cholangiocarcinoma	C04.557.470.200.025.450
D006330	Heart Defects, Congenital	C14.240.400; C14.280.400; C16.131.240.400

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL1783 (SINGLE PROTEIN), CHEMBL5482974 (PROTEIN-PROTEIN INTERACTION), CHEMBL5482995 (PROTEIN COMPLEX), CHEMBL5482996 (PROTEIN COMPLEX), CHEMBL5482997 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 2,881 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL3646221	VADADUSTAT	4	533
CHEMBL4585668	BELZUTIFAN	4	1,088
CHEMBL253969	OSI-632	2	1,150
CHEMBL3115298	IZILENDUSTAT	2	51
CHEMBL5314521	IMDATIFAN	2	59

Clinical evidence (CIViC)

Drug × variant × indication: 1 predictive associations from 1 curated evidence items.

Variant	Therapy	Indication	Effect	Level	CIViC
VEGFA Decreased Peri-therapeutic Expression	Levoleucovorin + Irinotecan + Bevacizumab + Fluorouracil	Colorectal Cancer	Sensitivity/Response	CIViC B	EID818

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

28 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs13207351	Efficacy	3	docetaxel	Breast Neoplasms
rs144854329	Efficacy	3	docetaxel	Breast Neoplasms
rs1570360	Efficacy	3	docetaxel	Breast Neoplasms
rs1570360	Efficacy	3	sorafenib	Renal Cell Carcinoma
rs1570360	Efficacy	3	cyclophosphamide;docetaxel	Prostatic Neoplasms
rs2010963	Efficacy	3	cyclophosphamide	Prostatic Neoplasms
rs2010963	Efficacy	3	bevacizumab;pegaptanib;ranibizumab	Choroidal Neovascularization
rs2010963	Toxicity	3	sorafenib	Hand-foot syndrome;Renal Cell Carcinoma
rs2010963	Efficacy	3	sorafenib	Hepatocellular Carcinoma
rs2010963	Efficacy	3	capecitabine;oxaliplatin	Colorectal Neoplasms
rs25648	Efficacy	3	cisplatin;fluorouracil;oxaliplatin	Stomach Neoplasms
rs3025000	Efficacy	3	bevacizumab;ranibizumab	Macular Degeneration
rs3025039	Efficacy	3	bevacizumab	Breast Neoplasms
rs3025039	Efficacy	3	bevacizumab	Breast Neoplasms;Colorectal Neoplasms
rs3025040	Toxicity	3	sorafenib	Hand-foot syndrome;Hepatocellular Carcinoma
rs35864111	Efficacy	3	docetaxel	Breast Neoplasms
rs6900017	Toxicity	3	carboplatin;taxanes	Ovarian Neoplasms
rs699947	Efficacy	3	sildenafil	Erectile Dysfunction
rs699947	Toxicity	3	sunitinib
rs699947	Efficacy	3	bevacizumab;capecitabine;fluorouracil;irinotecan;leucovorin;oxaliplatin	Colorectal Neoplasms
rs699947	Efficacy	3	enalapril	Hypertension
rs699947	Efficacy	4	ranibizumab	Macular Degeneration
rs699947	Efficacy	4	docetaxel	Breast Neoplasms
rs833061	Toxicity	3	sunitinib
rs833069	Efficacy	4	ranibizumab	Macular Degeneration
rs879825	Toxicity	3	carboplatin;taxanes	Ovarian Neoplasms
rs9369421	Efficacy	3	carboplatin;taxanes	Ovarian Neoplasms
rs9369421	Toxicity	3	carboplatin;taxanes

PharmGKB variants

24 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs7664413	VEGFA, VEGFC		0.00	0
rs10434	VEGFA		0.00	0
rs25648	VEGFA	3	2.75	1	cisplatin;fluorouracil;oxaliplatin
rs699946	VEGFA		0.00	0
rs699947	VEGFA	3	3.00	6	ranibizumab;sildenafil;sunitinib;docetaxel;bevacizumab;capecitabine;fluorouracil;irinotecan;leucovorin;oxaliplatin;enalapril
rs833061	VEGFA	3	2.00	1	sunitinib
rs833062	VEGFA		0.00	0
rs833069	VEGFA	4	-2.00	1	ranibizumab
rs879825	VEGFA	3	3.50	1	carboplatin;taxanes
rs1005230	VEGFA		0.00	0
rs1570360	VEGFA	3	3.50	3	cyclophosphamide;docetaxel;sorafenib;docetaxel
rs2010963	VEGFA	3	5.00	5	cyclophosphamide;sorafenib;bevacizumab;pegaptanib;ranibizumab;capecitabine;oxaliplatin
rs2146323	VEGFA		0.00	0
rs3025000	VEGFA	3	6.50	1	bevacizumab;ranibizumab
rs3025030	VEGFA		0.00	0
rs3025033	VEGFA		0.00	0
rs3025039	VEGFA	3	2.50	2	bevacizumab
rs6900017	VEGFA	3	3.00	1	carboplatin;taxanes
rs9369421	VEGFA	3	3.00	2	carboplatin;taxanes
rs13207351	VEGFA	3	2.25	1	docetaxel
rs35864111	VEGFA	3	2.25	1	docetaxel
rs144854329	VEGFA	3	2.25	1	docetaxel
rs3025040	VEGFA	3	1.75	1	sorafenib
rs833068	VEGFA		0.00	0

Binding affinities (BindingDB)

202 measured of 224 human assays (224 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(1S)-4-(3,5-difluorophenoxy)-2,2-difluoro-7-(fluoromethylsulfonyl)-1,3-dihydroinden-1-ol	EC50	1 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-2,2-difluoro-1-hydroxy-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	4 nM	US-9896418: Aryl ethers and uses thereof
7-(difluoromethylsulfonyl)-4-(3,5-difluorophenoxy)-2,2-difluoro-1,3-dihydroinden-1-ol	EC50	6 nM	US-9896418: Aryl ethers and uses thereof
(1S)-4-(3-chloro-5-fluorophenoxy)-7-(difluoromethylsulfonyl)-2,2-difluoro-1,3-dihydroinden-1-ol	EC50	6 nM	US-9896418: Aryl ethers and uses thereof
3-fluoro-5-[[(1S,3R)-2,2,3-trifluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]benzonitrile	EC50	6.2 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-2,2-difluoro-1-hydroxy-7-(trifluoromethyl)-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	6.2 nM	US-9896418: Aryl ethers and uses thereof
4-(3,5-difluorophenoxy)-2,2-difluoro-7-methylsulfonyl-1,3-dihydroinden-1-ol	EC50	7 nM	US-9896418: Aryl ethers and uses thereof
4-(Difluoromethyl)-5-(3,5-difluorophenoxy)-2,2- difluoro-3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide	EC50	9 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(3R)-5-(3-cyano-5-fluoro-phenoxy)-2,2- difluoro-3-hydroxy-3-methyl-1,1-dioxo- benzothiophene-4-carbonitrile	IC50	9 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
3-[(4-bromo-2,6-difluorophenyl)methoxy]-5-({[4-(pyrrolidin-1-yl)butyl]carbamoyl}amino)-1,2-thiazole-4-carboxamide	IC50	10.1 nM	US-9446026: Ocular formulations for drug-delivery to the posterior segment of the eye
5-(1-benzothiophen-4-yloxy)-4-(difluoromethyl)-2,2-difluoro-1,1-dioxo-3H-1-benzothiophen-3-ol	IC50	11 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(1S)-4-(3,5-difluorophenoxy)-2,2-difluoro-7-methylsulfonyl-1,3-dihydroinden-1-ol	EC50	11 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-7-(difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	13 nM	US-9896418: Aryl ethers and uses thereof
(1S)-4-[(5-chloro-3-pyridinyl)oxy]-2,2-difluoro-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-1-ol	EC50	13 nM	US-9896418: Aryl ethers and uses thereof
3-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1- dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)-5- fluorobenzonitrile	EC50	14 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
[[(1R,3S)-7-(3-cyano-5-fluorophenoxy)-1,2,2-trifluoro-3-hydroxy-1,3-dihydroinden-4-yl]-methyl-oxo-lambda6-sulfanylidene]cyanamide	EC50	14 nM	US-9896418: Aryl ethers and uses thereof
5-(3-chloro-5-fluorophenoxy)-2,2-difluoro-4-methyl-1,1-dioxo-3H-1-benzothiophen-3-ol	IC50	15 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
3-[[7-(difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	15 nM	US-9896418: Aryl ethers and uses thereof
(1S)-4-(3,4-difluorophenoxy)-2,2-difluoro-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-1-ol	EC50	15 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-7-(difluoromethylsulfonyl)-2,2-difluoro-1-hydroxy-1,3-dihydroinden-4-yl]oxy]benzonitrile	EC50	16 nM	US-9896418: Aryl ethers and uses thereof
(R)-3-((4-bromo-2,2-difluoro-3-hydroxy-1,1-dioxido- 2,3-dihydrobenzo[b]thiophen-5-yl)oxy)benzonitrile	IC50	17 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
5-(3,5-Difluorophenoxy)-2,2-difluoro-3- hydroxy-3-methyl-2,3- dihydrobenzo[b]thiophene-4-carbonitrile 1,1- dioxide	EC50	18 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
Belzutifan	EC50	18 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-2,2-difluoro-1-hydroxy-7-(trifluoromethylsulfonimidoyl)-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	19.2 nM	US-9896418: Aryl ethers and uses thereof
[4-(difluoromethyl)-5-(3,5-difluorophenoxy)-2,2-difluoro-3-hydroxy-1-oxo-3H-1-benzothiophen-1-ylidene]cyanamide	IC50	20 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
3-[[(1S)-2,2-difluoro-7-(fluoromethylsulfonyl)-1-hydroxy-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	20 nM	US-9896418: Aryl ethers and uses thereof
(R)-4-(Difluoromethyl)-5-(3,4-difluorophenoxy)-2,2- difluoro-3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide	IC50	24 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(1S)-2,2-difluoro-4-[(5-fluoro-3-pyridinyl)oxy]-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-1-ol	EC50	26 nM	US-9896418: Aryl ethers and uses thereof
5-[[(1S)-2,2-difluoro-1-hydroxy-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-4-yl]oxy]-2-fluorobenzonitrile	EC50	28 nM	US-9896418: Aryl ethers and uses thereof
5-[[(1S)-2,2-difluoro-1-hydroxy-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-4-yl]oxy]pyridine-3-carbonitrile	EC50	28 nM	US-9896418: Aryl ethers and uses thereof
5-(3-Chloro-5-fluorophenoxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide	EC50	29 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(1S)-2,2-difluoro-4-(4-fluorophenoxy)-7-(trifluoromethylsulfonyl)-1,3-dihydroinden-1-ol	EC50	29 nM	US-9896418: Aryl ethers and uses thereof
[(3S)-4-bromo-5-(3-chloro-5-fluorophenoxy)-1,1-dioxo-2,3-dihydro-1-benzothiophen-3-yl] (2S)-3,3,3-trifluoro-2-methoxy-2-phenylpropanoate	EC50	31 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(R)-3-Amino-4-(difluoromethyl)-5-(3,5- difluorophenoxy)-2,2-difluoro-2,3- dihydrobenzo[b]thiophene 1,1-dioxide	IC50	33 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
4-(3-chloro-5-fluorophenoxy)-7-(difluoromethylsulfonyl)-2,2-difluoro-1,3-dihydroinden-1-ol	EC50	33 nM	US-9896418: Aryl ethers and uses thereof
(R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy- 1,1-dioxido-2,3-dihydrobenzo[b]thiophen-5- yl)oxy)benzonitrile	IC50	34 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(1R)-4-(3,5-difluorophenoxy)-7-(trifluoromethylsulfonyl)-2,3-dihydro-1H-inden-1-ol	EC50	35 nM	US-9896418: Aryl ethers and uses thereof
(1S)-4-[(5-chloro-3-pyridinyl)oxy]-7-(difluoromethylsulfonyl)-2,2-difluoro-1,3-dihydroinden-1-ol	EC50	37 nM	US-9896418: Aryl ethers and uses thereof
3-chloro-5-[[(1S)-2,2-difluoro-7-(fluoromethylsulfonyl)-1-hydroxy-1,3-dihydroinden-4-yl]oxy]benzonitrile	EC50	38 nM	US-9896418: Aryl ethers and uses thereof
(1R)-4-(3,5-difluorophenoxy)-7-(fluoromethylsulfonyl)-2,3-dihydro-1H-inden-1-ol	EC50	40 nM	US-9896418: Aryl ethers and uses thereof
3-[[(1S)-2,2-difluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile	EC50	42 nM	US-9896418: Aryl ethers and uses thereof
5-(3-chloro-5-fluorophenoxy)-2,2-difluoro-3-hydroxy-1,1-dioxo-3H-1-benzothiophene-4-carbonitrile	IC50	45 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(R)-4-Bromo-5-(3-chloro-5-fluoro-phenoxy)-2,2- difluoro-1,1-dioxo-3H-benzothiophen-3-ol	EC50	45 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
5-(3,5-difluorophenoxy)-2,2-difluoro-3-hydroxy-1,1-dioxo-3H-1-benzothiophene-4-carbonitrile	IC50	46 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(3R)-5-(3-chloro-5-fluoro-phenoxy)-3-hydroxy-1,1- dioxo-2,3-dihydrobenzothiophene-4-carbonitrile	IC50	47 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(1S)-7-(difluoromethylsulfonyl)-4-(3,4-difluorophenoxy)-2,2-difluoro-1,3-dihydroinden-1-ol	EC50	47 nM	US-9896418: Aryl ethers and uses thereof
5-(3-cyano-5-fluoro-phenoxy)-2,2-difluoro-3- hydroxy-3-methyl-1,1-dioxo-benzothiophene- 4-carbonitrile	EC50	48 nM	US-9884843: Cyclic sulfone and sulfoximine analogs and uses thereof
(3S)-7-(3,5-difluorophenoxy)-2,2-difluoro-3-hydroxy-N-methyl-1,3-dihydroindene-4-sulfonamide	EC50	48 nM	US-9896418: Aryl ethers and uses thereof
3-chloro-5-[[(1S)-2,2-difluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]benzonitrile	EC50	50 nM	US-9896418: Aryl ethers and uses thereof
5-[[(1S,3R)-2,2,3-trifluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]pyridine-3-carbonitrile	EC50	52 nM	US-9896418: Aryl ethers and uses thereof

ChEMBL bioactivities

435 potent at pChembl≥5 of 531 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.60	Kd	0.025	nM	CHEMBL3219623
10.60	Kd	0.025	nM	CHEMBL3219622
10.34	Kd	0.046	nM	CHEMBL3219622
9.92	IC50	0.12	nM	CHEMBL3234202
9.52	IC50	0.3	nM	CHEMBL3234200
9.49	IC50	0.32	nM	APRATOXIN S4
9.33	IC50	0.47	nM	CHEMBL3234201
9.21	Kd	0.62	nM	CHEMBL604368
9.18	Kd	0.66	nM	S-ROLIPRAM
9.15	Kd	0.7	nM	CHEMBL590011
9.10	Kd	0.79	nM	CHEMBL604570
9.00	EC50	1	nM	CHEMBL5848806
8.85	Kd	1.4	nM	CHEMBL604568
8.82	Kd	1.5	nM	CHEMBL604366
8.77	Kd	1.7	nM	CHEMBL382044
8.77	Kd	1.7	nM	CHEMBL198643
8.74	Kd	1.8	nM	CHEMBL603122
8.70	IC50	2	nM	CHEMBL4165557
8.70	EC50	2	nM	CHEMBL5590666
8.66	Kd	2.2	nM	MUPARFOSTAT SODIUM
8.40	EC50	4	nM	CHEMBL4176457
8.29	Kd	5.1	nM	CHEMBL590013
8.28	IC50	5.27	nM	OSI-632
8.22	EC50	6	nM	CHEMBL5986684
8.22	EC50	6	nM	CHEMBL5801572
8.22	EC50	6	nM	IMDATIFAN
8.21	EC50	6.2	nM	CHEMBL4453227
8.21	EC50	6.2	nM	CHEMBL5951034
8.15	Kd	7.1	nM	CHEMBL265885
8.15	IC50	7	nM	CHEMBL6007442
8.15	EC50	7	nM	CHEMBL6025188
8.15	EC50	7	nM	CHEMBL5756693
8.15	Kd	7.1	nM	CHEMBL602307
8.14	Kd	7.2	nM	CHEMBL262707
8.05	Kd	9	nM	CHEMBL5433780
8.05	IC50	9	nM	CHEMBL5421065
8.05	IC50	9	nM	CHEMBL5954894
8.05	EC50	9	nM	CHEMBL4168513
8.05	EC50	9	nM	CHEMBL4175320
8.05	Kd	8.9	nM	CHEMBL590012
8.03	IC50	9.333	nM	CHEMBL5421065
8.00	EC50	10	nM	CHEMBL5770461
7.98	Kd	10.4	nM	CHEMBL602114
7.96	Kd	11	nM	CHEMBL5433780
7.96	IC50	11	nM	CHEMBL5843327
7.96	IC50	11	nM	CHEMBL5928031
7.96	EC50	11	nM	CHEMBL5794926
7.96	EC50	11	nM	CHEMBL5885954
7.92	Kd	12	nM	CHEMBL5433780
7.92	Kd	12	nM	CHEMBL590010

PubChem BioAssay actives

90 with measured affinity, of 213 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S,3S,5S,7S,10S,16S,19S,22S,27R)-16-[(2S)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-[(4-methoxyphenyl)methyl]-2,5,17,19,20-pentamethyl-8-oxa-29-thia-14,17,20,23,30-pentazatricyclo[25.2.1.010,14]triacont-1(30)-ene-9,15,18,21,24-pentone	1125817: Inhibition of VEGF-A production in human HCT116 cells after 12 hrs by alphaLISA assay	ic50	0.0001	uM
(2S,3S,5S,7S,10S,16S,19S,22S,27S)-16-[(2S)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-[(4-methoxyphenyl)methyl]-2,5,17,19,20-pentamethyl-8-oxa-29-thia-14,17,20,23,30-pentazatricyclo[25.2.1.010,14]triacont-1(30)-ene-9,15,18,21,24-pentone	1125817: Inhibition of VEGF-A production in human HCT116 cells after 12 hrs by alphaLISA assay	ic50	0.0003	uM
(3S,5S,7S,10S,16S,19S,22S,27S)-16-[(2S)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-[(4-methoxyphenyl)methyl]-5,17,19,20-tetramethyl-8-oxa-29-thia-14,17,20,23,30-pentazatricyclo[25.2.1.010,14]triacont-1(30)-ene-9,15,18,21,24-pentone	1125817: Inhibition of VEGF-A production in human HCT116 cells after 12 hrs by alphaLISA assay	ic50	0.0003	uM
(3S,5S,7S,10S,16S,19S,22S,27S)-16-[(2S)-butan-2-yl]-7-tert-butyl-3-hydroxy-22-[(4-methoxyphenyl)methyl]-2,2,5,17,19,20-hexamethyl-8-oxa-29-thia-14,17,20,23,30-pentazatricyclo[25.2.1.010,14]triacont-1(30)-ene-9,15,18,21,24-pentone	1125817: Inhibition of VEGF-A production in human HCT116 cells after 12 hrs by alphaLISA assay	ic50	0.0005	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-phenyltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0006	uM
(4S)-4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0007	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-naphthalen-1-yltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0007	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[12-(4-naphthalen-1-yltriazol-1-yl)dodecoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0008	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[3-(4-phenyltriazol-1-yl)propoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0014	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-octoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0015	uM
(2R,3S,4S,5S,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-phenylmethoxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol	256834: Binding affinity for VEGF by BIAcore solution affinity assay	kd	0.0017	uM
(2R,3S,4S,5S,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-octoxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol	256834: Binding affinity for VEGF by BIAcore solution affinity assay	kd	0.0017	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-phenylmethoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0018	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[12-(4-phenyltriazol-1-yl)dodecoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0051	uM
N-[(2S,3S,4S,5S,6R)-3-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[(2R,3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-2-phenoxyacetamide	256834: Binding affinity for VEGF by BIAcore solution affinity assay	kd	0.0071	uM
tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-naphthalen-1-yltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0071	uM
6-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-N-[(2S,3S,4S,5S,6R)-3-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[(2R,3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]hexanamide	256834: Binding affinity for VEGF by BIAcore solution affinity assay	kd	0.0072	uM
tridecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[8-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]octoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0089	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]-6-(diaminomethylideneamino)hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016518: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-2 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.0090	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0090	uM
tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-phenyltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0104	uM
tridecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[(4-butylphenyl)methoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0120	uM
hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-dodecoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0120	uM
hexadecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[3-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]propoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0122	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0150	uM
(3R,4S)-7’-(difluoromethoxy)-3,8-difluoro-6’,7-bis(trifluoromethyl)spiro[2,3-dihydrothiopyrano[3,2-c]pyridine-4,2’-3H-imidazo[1,2-a]pyridine]	2117105: Inhibition of VEGF (unknown origin) by FRET based analysis	ic50	0.0150	uM
(2R,3S)-8-[(2S,4R)-5,7-dihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-4-yl]-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol	730063: Binding affinity to recombinant VEGFA (unknown origin) measured for 60 seconds by surface plasmon resonance assay	kd	0.0160	uM
8-[5-(5,7-dihydroxy-4-oxochromen-2-yl)-2-hydroxyphenyl]-5,7-dihydroxy-2-(4-hydroxyphenyl)chromen-4-one	730063: Binding affinity to recombinant VEGFA (unknown origin) measured for 60 seconds by surface plasmon resonance assay	kd	0.0165	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0180	uM
tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-octoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0180	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0200	uM
tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-phenylmethoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0210	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0220	uM
tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[3-(4-phenyltriazol-1-yl)propoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate	459629: Binding affinity to VEGF by surface plasmon-based solution affinity assay	kd	0.0250	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[3-[4-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7,39-bis(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-13-yl]butylamino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0260	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.0390	uM
(1R,5R,6S,13S,21R)-13-(3,4-dihydroxyphenyl)-5-(4-hydroxyphenyl)-4,12,14-trioxapentacyclo[11.7.1.02,11.03,8.015,20]henicosa-2(11),3(8),9,15,17,19-hexaene-6,9,17,19,21-pentol	730063: Binding affinity to recombinant VEGFA (unknown origin) measured for 60 seconds by surface plasmon resonance assay	kd	0.0480	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-(4-acetamidobutyl)-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.0500	uM
(1aR,3S,7bR)-7-chloro-7’-(difluoromethoxy)-6’-(trifluoromethyl)spiro[1,1a,2,7b-tetrahydrocyclopropa[h]isoquinoline-3,2’-3H-imidazo[1,2-a]pyridine]	2117105: Inhibition of VEGF (unknown origin) by FRET based analysis	ic50	0.0500	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-13-(4-aminobutyl)-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.1290	uM
3-[(1S,4S,7S,10S,13S,16S,19S,22S,25S,28R,33R,36S,39S,42S)-28-acetamido-42-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl]-36-benzyl-22-[(2S)-butan-2-yl]-13-[4-[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-carboxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]butyl]-7-(2-carboxyethyl)-25-(carboxymethyl)-19-(1H-imidazol-5-ylmethyl)-4,10-bis(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,34,37,40,44,50-tetradecaoxo-16-propan-2-yl-30,31-dithia-2,5,8,11,14,17,20,23,26,35,38,41,45,51-tetradecazabicyclo[31.16.2]henpentacontan-39-yl]propanoic acid	1997504: Binding affinity to human VEGF (13 to 107 residues) expressed in Escherichia coli Rosetta (DE3) cells assessed as dissociation constant at 20 degreeC by isothermal titration calorimetry analysis	kd	0.1580	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-6-(diaminomethylideneamino)-2-[[(2S)-2,3-diaminopropanoyl]amino]hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.3288	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-[[(2S)-2,3-diaminopropanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.4345	uM
(1R,5R,6S,13S,21R)-5,13-bis(3,4-dihydroxyphenyl)-4,12,14-trioxapentacyclo[11.7.1.02,11.03,8.015,20]henicosa-2(11),3(8),9,15,17,19-hexaene-6,9,17,19,21-pentol	730063: Binding affinity to recombinant VEGFA (unknown origin) measured for 60 seconds by surface plasmon resonance assay	kd	0.4760	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-2-[[(2S)-2-amino-4-sulfanylbutanoyl]amino]-6-(diaminomethylideneamino)hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.6266	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-[[(2S)-2-amino-4-sulfanylbutanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.6982	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-6-(diaminomethylideneamino)hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.8100	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-[[(2S)-2-amino-5-sulfanylpentanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	0.8900	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-(3-sulfanylpropanoylamino)hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	1.1220	uM
(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-2-[[(2S)-2-amino-5-sulfanylpentanoyl]amino]-6-(diaminomethylideneamino)hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid	2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA	ic50	1.3183	uM

CTD chemical–gene interactions

682 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Oxygen	decreases reaction, increases secretion, increases expression, affects cotreatment, affects expression (+6 more)	64
cobaltous chloride	decreases reaction, increases secretion, affects reaction, affects binding, increases reaction (+6 more)	53
Resveratrol	decreases expression, increases expression, increases reaction, decreases secretion, decreases response to substance (+6 more)	33
sodium arsenite	decreases reaction, increases expression, increases secretion, affects reaction, affects cotreatment (+4 more)	28
Arsenic Trioxide	increases expression, increases reaction, decreases response to substance, decreases reaction, decreases secretion (+4 more)	18
Acetylcysteine	decreases reaction, increases expression, decreases secretion, decreases expression, increases abundance (+4 more)	17
bisphenol A	increases methylation, increases reaction, increases secretion, decreases expression, increases expression (+4 more)	16
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one	increases expression, increases secretion, increases abundance, increases reaction, decreases expression (+2 more)	16
Particulate Matter	decreases phosphorylation, decreases secretion, decreases reaction, increases abundance, decreases expression (+3 more)	16
Curcumin	affects cotreatment, decreases reaction, increases phosphorylation, affects expression, increases expression (+5 more)	15
Estradiol	decreases reaction, increases secretion, increases expression, affects cotreatment, increases reaction (+1 more)	14
Quercetin	increases reaction, increases expression, increases localization, decreases expression, decreases reaction (+3 more)	14
Tobacco Smoke Pollution	decreases activity, decreases reaction, affects cotreatment, decreases expression, increases secretion (+4 more)	12
SB 203580	decreases reaction, increases expression, increases secretion, decreases expression, decreases secretion	11
U 0126	decreases reaction, increases expression, increases secretion, affects reaction, increases abundance (+1 more)	11
Wortmannin	decreases secretion, affects cotreatment, decreases reaction, increases expression, increases secretion	10
Doxorubicin	decreases expression, increases reaction, affects reaction, decreases reaction, decreases response to substance (+2 more)	10
Glucose	increases expression, increases reaction, affects cotreatment, decreases expression, increases secretion (+1 more)	10
Lipopolysaccharides	decreases expression, affects reaction, decreases reaction, increases expression, affects cotreatment (+2 more)	10
Cisplatin	decreases abundance, affects binding, affects cotreatment, increases expression, increases reaction (+3 more)	9
Tetrachlorodibenzodioxin	decreases reaction, increases expression, affects cotreatment	9
Thalidomide	affects cotreatment, decreases expression, decreases reaction, decreases secretion, affects expression (+3 more)	9
Nicotine	decreases reaction, increases expression, affects reaction, decreases secretion, increases secretion	8
Tretinoin	decreases secretion, affects cotreatment, decreases reaction, increases secretion, increases expression (+2 more)	8
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one	decreases expression, decreases phosphorylation, decreases secretion, decreases reaction, increases secretion (+2 more)	7
Deferoxamine	affects cotreatment, increases expression, affects binding, increases reaction, decreases reaction	7
Cadmium Chloride	increases reaction, decreases reaction, increases expression, affects reaction, affects expression (+1 more)	7
methylmercuric chloride	increases secretion, affects cotreatment, decreases reaction, increases expression, decreases expression	6
epigallocatechin gallate	decreases secretion, affects cotreatment, decreases reaction, increases expression, increases reaction (+1 more)	6
deguelin	decreases reaction, increases expression, decreases expression, decreases response to substance	6

ChEMBL screening assays

64 unique, capped per target: 64 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1072348	Binding	Binding affinity to VEGF by surface plasmon-based solution affinity assay	Synthesis and biological evaluation of polysulfated oligosaccharide glycosides as inhibitors of angiogenesis and tumor growth. — J Med Chem

Cellosaurus cell lines

12 cell lines: 7 cancer cell line, 3 embryonic stem cell, 2 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_6503	MS1 VEGF	Transformed cell line	Sex unspecified
CVCL_A7T9	SEES3-1V human VEGFA, clone1	Embryonic stem cell	Male
CVCL_A7U0	SEES3-1V human VEGFA, clone2	Embryonic stem cell	Male
CVCL_A7U1	SEES3-1V human VEGFA, clone3	Embryonic stem cell	Male
CVCL_B2L1	Abcam HeLa VEGFA KO	Cancer cell line	Female
CVCL_B8RM	Abcam HCT 116 VEGFA KO	Cancer cell line	Male
CVCL_B9U2	Abcam A-549 VEGFA KO	Cancer cell line	Male
CVCL_D2HN	Abcam MCF-7 VEGFA KO	Cancer cell line	Female
CVCL_D8Y3	Ubigene HCT 116 VEGFA KO	Cancer cell line	Male
CVCL_D9VM	Ubigene HEK293 VEGFA KO	Transformed cell line	Female

Clinical trials (associated diseases)

600 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00668824	PHASE4	UNKNOWN	Improved Diagnosis of Congenital Heart Disease by Magnetic Resonance Imaging Using Vasovist
NCT01368705	PHASE4	COMPLETED	Nitrogen Balance in Infants After Post Cardiothoracic Surgery
NCT01619982	PHASE4	COMPLETED	Pre-operative Prophylaxis With Vancomycin and Cefazolin in Pediatric Cardiovascular Surgery Patients
NCT02122679	PHASE4	WITHDRAWN	Tranexamic Acid Effect on Platelet Aggregation Following Infant Cardiopulmonary Bypass
NCT02527811	PHASE4	UNKNOWN	Ulinastatin Injection in in Pediatric Patients Undergoing Open Heart Surgery
NCT03014700	PHASE4	COMPLETED	Fibrinogen Concentrate vs Cryoprecipitate
NCT03408340	PHASE4	TERMINATED	Paravertebral Nerve Blocks in Neonates
NCT03630796	PHASE4	UNKNOWN	Effect of Sevoflurane in Postoperative Troponin I Levels in Children Undergoing Congenital Heart Defects Surgery
NCT03667703	PHASE4	COMPLETED	Stress Ulcer Prophylaxis Versus Placebo in Critically Ill Infants With Congenital Heart Disease
NCT04453761	PHASE4	UNKNOWN	Thiamine Influenced on Substrate Energy Effectiveness in Indonesian Children Undergoing Cardiopulmonary Bypass
NCT06668389	PHASE4	RECRUITING	Sodium-Glucose Cotransporter 2 Inhibitors for Repaired Tetralogy of Fallot Patients for Enhancement of Cardio-Pulmonary Status Trial
NCT07499154	PHASE4	NOT_YET_RECRUITING	Perioperative Lidocaine for Lung Protection in Infants Undergoing Cardiac Surgery
NCT00168987	PHASE4	COMPLETED	Influence of an Oral Nutritional Supplement Rich in Omega-3 Fatty Acids on Functional State and Quality of Life in Malnourished Patients With Gastroenterological Tumors
NCT00280709	PHASE4	COMPLETED	Biliary Metal Stent Study: Metal Stents for Management of Distal Malignant Biliary Obstruction
NCT00797121	PHASE4	UNKNOWN	Preoperative Biliary Drainage for Resectable Hilar Cholangiocarcinoma
NCT01111591	PHASE4	UNKNOWN	Cyclooxygenase-2 Inhibitor for Adjuvant Anticancer Effect in Patients With Biliary-pancreas Cancer
NCT01256034	PHASE4	COMPLETED	Effects of Preoperative Immunonutrition in Patients Undergoing Pancreaticoduodenectomy
NCT01256047	PHASE4	COMPLETED	Effects of Preoperative Immunonutrition in Patients Undergoing Hepatectomy
NCT01642875	PHASE4	UNKNOWN	Early Oral Versus Enteral Nutrition After Pancreatoduodenectomy
NCT02027311	PHASE4	COMPLETED	Etomidate vs. Midazolam for Sedation During ERCP
NCT02174575	PHASE4	WITHDRAWN	Anesthetic Agents and Acute Kidney Injury After Liver Resection Surgery
NCT07486713	PHASE4	RECRUITING	Olutasidenib DDI Study in Patients With IDH1 Mutation Positive Malignancies
NCT00000470	PHASE3	COMPLETED	Infant Heart Surgery: Central Nervous System Sequelae of Circulatory Arrest
NCT00000494	PHASE3	COMPLETED	Management of Patent Ductus in Premature Infants
NCT01134302	PHASE3	UNKNOWN	Hybrid Versus Norwood Management Strategies in Infants Undergoing Single Ventricle Palliation
NCT01607983	PHASE3	WITHDRAWN	Effects of Pulmonary Vasodilation Upon VA Coupling in Fontan Patients
NCT01662011	PHASE3	UNKNOWN	Application of Neurally Adjusted Ventilatory Assist to Children After Congenital Cardiac Surgery
NCT02320669	PHASE3	COMPLETED	Phase 3 Triiodothyronine Supplementation for Infants After Cardiopulmonary Bypass
NCT02615262	PHASE3	COMPLETED	Intraoperative Dexamethasone in Pediatric Cardiac Surgery
NCT03153137	PHASE3	COMPLETED	Clinical Study Assessing the Efficacy and Safety of Macitentan in Fontan-palliated Subjects
NCT03154476	PHASE3	COMPLETED	Role of Sildenafil for Fontan Associated Liver Disease (SiFALD) Study
NCT04536194	PHASE3	COMPLETED	Dopamine Versus Norepinephrine Under General Anesthesia
NCT04702373	PHASE3	ACTIVE_NOT_RECRUITING	Training in Exercise Activities and Motion for Growth (TEAM 4 Growth) RCT
NCT05049590	PHASE3	COMPLETED	Acute Normovolemic Hemodilution in Complex Cardiac Surgery
NCT06406517	PHASE3	UNKNOWN	Comparative Effectiveness of Gadopiclenol for Evaluation of Adult Congenital Heart Anatomy and Hemodynamics
NCT06693674	PHASE3	RECRUITING	Effect of Sacubitril-Valsartan on Cardiac Structure and Function
NCT06955260	PHASE3	NOT_YET_RECRUITING	SGLT2 Inhibition With Empagliflozin in Fontan Circulatory Failure
NCT00540735	PHASE3	TERMINATED	Efficiency Evaluation of Photodynamic Therapy With Photofrin® on Unresectable Type III or IV Cholangiocarcinomas
NCT00653978	PHASE3	UNKNOWN	Unilateral Versus Bilateral Stents for Bismuth Type II and III Malignant Hilar Strictures
NCT00809081	PHASE3	UNKNOWN	Early Enteral Feeding After Pylorus Preserving Pancreatoduodenectomy