NRP1
gene geneOn this page
Also known as NRPVEGF165RCD304
Summary
NRP1 (neuropilin 1, HGNC:8004) is a protein-coding gene on chromosome 10p11.22, encoding Neuropilin-1 (O14786). Cell-surface receptor involved in the development of the cardiovascular system, in angiogenesis, in the formation of certain neuronal circuits and in organogenesis outside the nervous system.
This gene encodes one of two neuropilins, which contain specific protein domains which allow them to participate in several different types of signaling pathways that control cell migration. Neuropilins contain a large N-terminal extracellular domain, made up of complement-binding, coagulation factor V/VIII, and meprin domains. These proteins also contains a short membrane-spanning domain and a small cytoplasmic domain. Neuropilins bind many ligands and various types of co-receptors; they affect cell survival, migration, and attraction. Some of the ligands and co-receptors bound by neuropilins are vascular endothelial growth factor (VEGF) and semaphorin family members. This protein has also been determined to act as a co-receptor for SARS-CoV-2 (which causes COVID-19) to infect host cells.
Source: NCBI Gene 8829 — RefSeq curated summary.
At a glance
- Gene–disease (curated): congenital heart disease (Limited, ClinGen)
- GWAS associations: 19
- Clinical variants (ClinVar): 326 total
- Druggable target: yes
- MANE Select transcript:
NM_003873
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:8004 |
| Approved symbol | NRP1 |
| Name | neuropilin 1 |
| Location | 10p11.22 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | NRP, VEGF165R, CD304 |
| Ensembl gene | ENSG00000099250 |
| Ensembl biotype | protein_coding |
| OMIM | 602069 |
| Entrez | 8829 |
Gene structure
Transcript identifiers
Ensembl transcripts: 30 — 30 protein_coding
ENST00000265371, ENST00000374816, ENST00000374821, ENST00000374822, ENST00000374823, ENST00000374867, ENST00000374875, ENST00000395995, ENST00000413802, ENST00000418675, ENST00000431894, ENST00000432372, ENST00000455749, ENST00000466932, ENST00000897563, ENST00000897564, ENST00000897565, ENST00000949861, ENST00000949862, ENST00000949863, ENST00000949864, ENST00000949865, ENST00000949866, ENST00000949867, ENST00000949868, ENST00000949869, ENST00000949870, ENST00000949871, ENST00000949872, ENST00000949873
RefSeq mRNA: 6 — MANE Select: NM_003873
NM_001024628, NM_001024629, NM_001244972, NM_001244973, NM_001330068, NM_003873
CCDS: CCDS31179, CCDS31180, CCDS7177, CCDS81448
Canonical transcript exons
ENST00000374867 — 17 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003692282 | 33330708 | 33330882 |
| ENSE00003843830 | 33177493 | 33180365 |
| ENSE00003846627 | 33334310 | 33334667 |
| ENSE00003889264 | 33207572 | 33207716 |
| ENSE00003889307 | 33185628 | 33185724 |
| ENSE00003889874 | 33263646 | 33263873 |
| ENSE00003889907 | 33256316 | 33256471 |
| ENSE00003890459 | 33226134 | 33226289 |
| ENSE00003890797 | 33186217 | 33186488 |
| ENSE00003891573 | 33192281 | 33192418 |
| ENSE00003891852 | 33202891 | 33202995 |
| ENSE00003892288 | 33213386 | 33213717 |
| ENSE00003892454 | 33254028 | 33254194 |
| ENSE00003892644 | 33270675 | 33270856 |
| ENSE00003895271 | 33182698 | 33182748 |
| ENSE00003895454 | 33221719 | 33221863 |
| ENSE00003896141 | 33197650 | 33197709 |
Expression profiles
Bgee: expression breadth ubiquitous, 279 present calls, max score 98.56.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 77.0172 / max 1881.7679, expressed in 1640 samples.
FANTOM5 promoters (15 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 109064 | 24.5275 | 1531 |
| 109061 | 18.3302 | 1511 |
| 109058 | 13.6480 | 1326 |
| 109060 | 4.7502 | 1173 |
| 109059 | 4.6143 | 1099 |
| 109063 | 2.6997 | 1088 |
| 109062 | 2.6773 | 1009 |
| 109069 | 1.6882 | 1090 |
| 109065 | 1.4150 | 762 |
| 109067 | 0.9138 | 606 |
Top tissues by expression
299 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| stromal cell of endometrium | CL:0002255 | 98.56 | gold quality |
| pericardium | UBERON:0002407 | 98.19 | gold quality |
| calcaneal tendon | UBERON:0003701 | 97.27 | gold quality |
| peritoneum | UBERON:0002358 | 96.96 | gold quality |
| omental fat pad | UBERON:0010414 | 96.96 | gold quality |
| synovial joint | UBERON:0002217 | 96.79 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 96.79 | gold quality |
| adrenal tissue | UBERON:0018303 | 96.36 | gold quality |
| heart right ventricle | UBERON:0002080 | 96.04 | gold quality |
| colonic epithelium | UBERON:0000397 | 96.01 | gold quality |
| gall bladder | UBERON:0002110 | 96.01 | gold quality |
| cardiac ventricle | UBERON:0002082 | 95.97 | gold quality |
| heart left ventricle | UBERON:0002084 | 95.94 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 95.94 | gold quality |
| adipose tissue | UBERON:0001013 | 95.78 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 95.65 | gold quality |
| metanephros cortex | UBERON:0010533 | 95.40 | gold quality |
| connective tissue | UBERON:0002384 | 95.32 | gold quality |
| superficial temporal artery | UBERON:0001614 | 95.29 | gold quality |
| heart | UBERON:0000948 | 95.15 | gold quality |
| apex of heart | UBERON:0002098 | 95.11 | gold quality |
| placenta | UBERON:0001987 | 94.98 | gold quality |
| cauda epididymis | UBERON:0004360 | 94.88 | gold quality |
| vena cava | UBERON:0004087 | 94.81 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 94.71 | gold quality |
| islet of Langerhans | UBERON:0000006 | 94.65 | gold quality |
| right atrium auricular region | UBERON:0006631 | 94.53 | gold quality |
| sural nerve | UBERON:0015488 | 94.52 | gold quality |
| cardiac atrium | UBERON:0002081 | 94.50 | gold quality |
| tendon | UBERON:0000043 | 94.42 | gold quality |
Single-cell (SCXA)
Detected in 16 experiment(s), a significant marker in 16.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-GEOD-98556 | yes | 373.03 |
| E-GEOD-130473 | yes | 313.07 |
| E-MTAB-7008 | yes | 126.22 |
| E-MTAB-6678 | yes | 38.75 |
| E-GEOD-135922 | yes | 21.65 |
| E-HCAD-9 | yes | 15.89 |
| E-MTAB-8271 | yes | 15.17 |
| E-CURD-112 | yes | 14.84 |
| E-CURD-119 | yes | 13.49 |
| E-GEOD-93593 | yes | 12.37 |
| E-MTAB-5061 | yes | 10.85 |
| E-MTAB-9067 | yes | 8.27 |
| E-MTAB-9801 | yes | 7.81 |
| E-GEOD-83139 | yes | 7.29 |
| E-ENAD-27 | yes | 6.58 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
1 targets.
| Target | Regulation |
|---|---|
| PHACTR1 | Activation |
Upstream regulators (CollecTRI, top): AR, ATF4, DLL4, E2F1, EMX1, ESR1, ETS1, EYA1, HAND2, MAX, NFE2L2, NOTCH1, NR2F2, NR4A2, PAX3, PROX1, REST, SP1, SSRP1, TFAP2A
Literature-anchored findings (GeneRIF, showing 40)
- A potential mechanism involved in hemangioma formation is the alteration of the NRP1 signaling pathway in endothelial and/or pericytic cells. (PMID:11807987)
- A neuronal receptor, neuropilin-1, is essential for the initiation of the primary immune response. (PMID:11953749)
- Neuropilin-1 is another neuronal molecule in the “immunological synapse”. (PMID:11976715)
- results suggest that NRP-1 may be a multiple function protein in human breast and may be involved in the induction of local invasiveness of neoplasia and angiogenesis and have direct relevance to the progression of breast cancer (PMID:12216067)
- promoter regions of human and mouse NRP1 genes were cloned and sequenced; transfection demonstrated that two Sp1 elements are major contributors to constitutive and induced activity (PMID:12577308)
- human glioma cells express class 3 semaphorins and receptors for soluble and membrane-bound semaphorins, suggesting a possible role of the semaphorin/neuropilin system in the interactions of human malignant glioma with the nervous and immune systems. (PMID:12730958)
- neuropilin-1 is expressed in the prostatic stromal cells, not epithelial tumor cells, and this expression is significantly increased in the malignant phenotype (PMID:12883660)
- breast carcinoma cells support an autocrine pathway involving SEMA3A, plexin-A1, and neuropilin-1 that impedes their ability to chemotax. (PMID:14500350)
- independently promote cell signaling in endothelial cells and also demonstrate the importance of last three amino acids for its function (PMID:14514674)
- Np-1 and Np-2 contribute to autocrine-paracrine interactions in pancreatic cancer (PMID:14760080)
- NP-1 has a specific role in mediating neurotrophic actions of VEGF family members (PMID:15126502)
- NRP1 overexpression contributes to tumor progression and has clinical significance for glioma. (PMID:15160992)
- Effect of NRP-1 overexpression on angiogenesis and growth of human colon adenocarcinoma by immunohistochemistry and in situ hybridization. (PMID:15161648)
- Increased expression of NRP1 is associated with an aggressive angiogenic phenotype in melanoma. (PMID:15166498)
- correlation between neuropilin-1 and vascularity in human astrocytic tumors and a possible role for neuropilin-1 as a receptor for VEGF-induced angiogenesis (PMID:15233640)
- dual role as an enhancer of VEGF activity and a mediator of endothelial cell adhesiveness (PMID:15522955)
- NP-1 mRNA was highly expressed in vascular endothelium and in stromal cells, but in these cells, NP-1 expression did not change during the menstrual cycle. (PMID:15613413)
- role for Npn-1 in regulating endothelial barrier dysfunction in response to VEGF. (PMID:15920019)
- Neuropilin-1 overexpression in pancreatic cancer cell lines is associated with (a) increased constitutive MAPK signalling, (b) inhibition of anoikis, and (c) chemoresistance (PMID:15956974)
- Down-regulation of NRP1 by NRSF overexpression reduced Sema3A activity. It was concluded that NRSF is a transcription factor that silences NRP1 expression and thereby diminishes the Sema3A mediated inhibition of HaCaT keratinocyte migration (PMID:16330548)
- Data show that tuftsin and a higher affinity antagonist, TKPPR, bind selectively to neuropilin-1 and block vascular endothelial growth factor (VEGF) binding to that receptor. (PMID:16371354)
- Preferential receptor binding and internalization by a ligand are mechanisms by which the common receptor Npn-1 can play an essential role in prioritizing conflicting signals. (PMID:16424390)
- This study describes the first specific antagonist of VEGF-A165 binding to NP-1 and demonstrate that NP-1 is essential for optimum KDR activation and intracellular signaling. (PMID:16513643)
- Immunohistochemical staining showed that NRP-1 was mainly confined to stroma and blood vessels and only in late-proliferative endometrium, epithelial staining was also observed. (PMID:16648151)
- GAG modification of NRP1 plays a critical role in modulating VEGF signaling, and may provide new insights into physiological and pathological angiogenesis. (PMID:16763549)
- NRP1 is involved in HTLV-1 and HTLV-2 entry (PMID:16809290)
- depletion of neuropilin-1 production by aortic smooth muscle cells with specific short hairpin RNA prevents the PDGF-dependent migration of vascular smooth muscle cells (PMID:16847823)
- NRP1 transfer to T lymphocytes during the immune synapse can convert T lymphocytes into vascular endothelial growth factor (VEGF)165-carrying cells. (PMID:16849452)
- increased NRP-1 expression in acute myeloid leukemia with significant correlation to survival (PMID:16990775)
- down-regulation of the neuropilin-1 transcripts by short interfering RNA caused spontaneous synoviocyte apoptosis, which was associated with both the decrease in Bcl-2 expression and the increase in Bax translocation to mitochondria. (PMID:17015762)
- Neuropilin-1 was expressed in most of human laryngeal carcinoma specimens and cell lines but was not expressed in nonmalignant tissue. (PMID:17017185)
- These results suggest that the expression of VEGFRs and NRPs on keratinocytes may constitute important regulators for its activity and may possibly be responsible for the autocrine signaling in the epidermis. (PMID:17088944)
- NP-1/Sema-3A-mediated interactions participate in the control of human thymocyte development (PMID:17369353)
- Data suggest that tumor cell-expressed NRP1 promotes glioma progression through potentiating the activity of the HGF/SF autocrine c-Met signaling pathway and enhancing angiogenesis. (PMID:17369861)
- NRP-1 expression was augmented threefold during malignant transformation of ovarian epithelial cells with oncogene ras, suggesting an association between NRP-1 and oncogenesis. (PMID:17376520)
- VEGF(121) binds directly to NRP1; however, unlike VEGF(165), VEGF(121) is not sufficient to bridge the NRP1.VEGFR2 complex. (PMID:17575273)
- Np-1 confers a growth and survival advantage to pancreas cancer cells, and interacts with integrin beta1 to coordinate signaling events that promote cell adherence and invasiveness. (PMID:17726369)
- neoplastic cells in myeloid leukemias frequently express VEGFR including NRP-1 and NRP-2 (PMID:17917967)
- These findings indicate that Np-1 is required for efficient activation of c-Met-dependent pathways that promote cell invasiveness. (PMID:17974973)
- This study, by elucidating the mechanisms that govern VPF/VEGF-induced EC survival signaling via NRP-1, contributes to a better understanding of molecular mechanisms of cardiovascular development (PMID:18000534)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | nrp1a | ENSDARG00000102153 |
| mus_musculus | Nrp1 | ENSMUSG00000025810 |
| rattus_norvegicus | Nrp1 | ENSRNOG00000010744 |
Paralogs (35): NRXN3 (ENSG00000021645), TLL1 (ENSG00000038295), CP (ENSG00000047457), DCBLD2 (ENSG00000057019), HEPH (ENSG00000089472), TLL2 (ENSG00000095587), PCOLCE (ENSG00000106333), CNTNAP3 (ENSG00000106714), CUBN (ENSG00000107611), CNTNAP1 (ENSG00000108797), NRXN2 (ENSG00000110076), MEP1A (ENSG00000112818), NRP2 (ENSG00000118257), CUZD1 (ENSG00000138161), MFGE8 (ENSG00000140545), MEP1B (ENSG00000141434), PDGFC (ENSG00000145431), CNTNAP4 (ENSG00000152910), CNTNAP3B (ENSG00000154529), CNTNAP5 (ENSG00000155052), CDCP2 (ENSG00000157211), PCOLCE2 (ENSG00000163710), EDIL3 (ENSG00000164176), NETO1 (ENSG00000166342), BMP1 (ENSG00000168487), PDGFD (ENSG00000170962), NETO2 (ENSG00000171208), CNTNAP2 (ENSG00000174469), NRXN1 (ENSG00000179915), HEPHL1 (ENSG00000181333), F8 (ENSG00000185010), ASTL (ENSG00000188886), F5 (ENSG00000198734), MFRP (ENSG00000235718), CNTNAP3C (ENSG00000283378)
Protein
Protein identifiers
Neuropilin-1 — O14786 (reviewed: O14786)
Alternative names: Vascular endothelial cell growth factor 165 receptor
All UniProt accessions (11): O14786, E7EX60, E9PEP6, H0Y4A0, H0Y4N6, H0Y7Z2, Q5JWQ2, Q5JWQ4, Q5JWQ6, Q5T7F0, V9GYL7
UniProt curated annotations — full annotation on UniProt →
Function. Cell-surface receptor involved in the development of the cardiovascular system, in angiogenesis, in the formation of certain neuronal circuits and in organogenesis outside the nervous system. Mediates the chemorepulsant activity of semaphorins. Recognizes a C-end rule (CendR) motif R/KXXR/K on its ligands which causes cellular internalization and vascular leakage. It binds to semaphorin 3A, the PLGF-2 isoform of PGF, the VEGF165 isoform of VEGFA and VEGFB. Coexpression with KDR results in increased VEGF165 binding to KDR as well as increased chemotaxis. Regulates VEGF-induced angiogenesis. Binding to VEGFA 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. Regulates mitochondrial iron transport via interaction with ABCB8/MITOSUR. (Microbial infection) Acts as a host factor for human coronavirus SARS-CoV-2 infection. Recognizes and binds to CendR motif RRAR on SARS-CoV-2 spike protein S1 which enhances SARS-CoV-2 infection. Binds VEGF-165 and may inhibit its binding to cells. May induce apoptosis by sequestering VEGF-165. May bind as well various members of the semaphorin family. Its expression has an averse effect on blood vessel number and integrity.
Subunit / interactions. Homodimer, and heterodimer with NRP2. Interacts with FER. Interacts with PLXNB1. Interacts with VEGFA. Interacts with ABCB8/MITOSUR in mitochondria. (Microbial infection) Interacts with SARS coronavirus-2/SARS-CoV-2 spike protein S1 (via the CendR motif RRAR).
Subcellular location. Secreted Mitochondrion membrane. Cell membrane. Cytoplasm.
Tissue specificity. The expression of isoforms 1 and 2 does not seem to overlap. Expressed in olfactory epithelium (at protein level). Expressed in fibroblasts (at protein level). Expressed by the blood vessels of different tissues. In the developing embryo it is found predominantly in the nervous system. In adult tissues, it is highly expressed in heart and placenta; moderately in lung, liver, skeletal muscle, kidney and pancreas; and low in adult brain. Expressed in the central nervous system, including olfactory related regions such as the olfactory tubercles and paraolfactory gyri. The expression of isoforms 1 and 2 does not seem to overlap. Found in liver hepatocytes, kidney distal and proximal tubules.
Domain organisation. The tandem CUB domains mediate binding to semaphorin, while the tandem F5/8 domains are responsible for heparin and VEGF binding. F5/8 domains mediate the recognition and binding to R/KXXR/K CendR motifs.
Similarity. Belongs to the neuropilin family.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O14786-1 | 1, Membrane-bound | yes |
| O14786-2 | 2, Soluble, SNRP1 | |
| O14786-3 | 3 |
RefSeq proteins (6): NP_001019799, NP_001019800, NP_001231901, NP_001231902, NP_001316997, NP_003864* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000421 | FA58C | Domain |
| IPR000859 | CUB_dom | Domain |
| IPR000998 | MAM_dom | Domain |
| IPR008979 | Galactose-bd-like_sf | Homologous_superfamily |
| IPR013320 | ConA-like_dom_sf | Homologous_superfamily |
| IPR014648 | Neuropilin | Family |
| IPR022579 | Neuropilin_C | Domain |
| IPR035914 | Sperma_CUB_dom_sf | Homologous_superfamily |
| IPR050633 | Neuropilin_MCO_CoagFactor | Family |
Pfam: PF00431, PF00629, PF00754, PF11980
UniProt features (101 total): strand 41, turn 12, helix 9, glycosylation site 8, disulfide bond 6, domain 5, sequence conflict 4, binding site 3, splice variant 3, sequence variant 3, topological domain 2, signal peptide 1, chain 1, region of interest 1, modified residue 1, transmembrane region 1
Structure
Experimental structures (PDB)
25 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6FMC | X-RAY DIFFRACTION | 0.9 |
| 6TKK | X-RAY DIFFRACTION | 1.06 |
| 8PFE | X-RAY DIFFRACTION | 1.35 |
| 5JGI | X-RAY DIFFRACTION | 1.38 |
| 5C7G | X-RAY DIFFRACTION | 1.45 |
| 5IJR | X-RAY DIFFRACTION | 1.52 |
| 9EOU | X-RAY DIFFRACTION | 1.55 |
| 7O1N | X-RAY DIFFRACTION | 1.56 |
| 9F6B | X-RAY DIFFRACTION | 1.57 |
| 5IYY | X-RAY DIFFRACTION | 1.6 |
| 5JGQ | X-RAY DIFFRACTION | 1.6 |
| 7P5U | X-RAY DIFFRACTION | 1.6 |
| 4RN5 | X-RAY DIFFRACTION | 1.73 |
| 2QQI | X-RAY DIFFRACTION | 1.8 |
| 5JHK | X-RAY DIFFRACTION | 1.8 |
| 1KEX | X-RAY DIFFRACTION | 1.9 |
| 2QQM | X-RAY DIFFRACTION | 2 |
| 5J1X | X-RAY DIFFRACTION | 2.1 |
| 2QQN | X-RAY DIFFRACTION | 2.2 |
| 5L73 | X-RAY DIFFRACTION | 2.24 |
| 7JJC | X-RAY DIFFRACTION | 2.36 |
| 4DEQ | X-RAY DIFFRACTION | 2.65 |
| 8C5G | X-RAY DIFFRACTION | 2.7 |
| 6FMF | X-RAY DIFFRACTION | 2.81 |
| 3I97 | X-RAY DIFFRACTION | 2.9 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O14786-F1 | 79.83 | 0.47 |
Antibody-complex structures (SAbDab): 1 — 2QQN
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (3): 195; 209; 250
Post-translational modifications (1): 894
Disulfide bonds (6): 27–54, 82–104, 147–173, 206–228, 275–424, 431–583
Glycosylation sites (8): 150, 261, 300, 522, 612, 612, 829, 842
Function
Pathways and Gene Ontology
Reactome pathways
8 pathways
| ID | Pathway |
|---|---|
| R-HSA-194306 | Neuropilin interactions with VEGF and VEGFR |
| R-HSA-376176 | Signaling by ROBO receptors |
| R-HSA-399954 | Sema3A PAK dependent Axon repulsion |
| R-HSA-399955 | SEMA3A-Plexin repulsion signaling by inhibiting Integrin adhesion |
| R-HSA-399956 | CRMPs in Sema3A signaling |
| R-HSA-445144 | Signal transduction by L1 |
| R-HSA-447041 | CHL1 interactions |
| R-HSA-9694614 | Attachment and Entry |
MSigDB gene sets: 938 (showing top):
GOBP_CARDIAC_CHAMBER_DEVELOPMENT, GOBP_PLATELET_DERIVED_GROWTH_FACTOR_RECEPTOR_SIGNALING_PATHWAY, GOBP_FOREBRAIN_NEURON_DEVELOPMENT, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_DENDRITE_DEVELOPMENT, MODULE_92, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, BERENJENO_ROCK_SIGNALING_NOT_VIA_RHOA_DN, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, AAGCAAT_MIR137, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT, GOBP_NEURON_RECOGNITION, GOBP_ACTIN_FILAMENT_BUNDLE_ORGANIZATION, GOBP_CARDIAC_SEPTUM_DEVELOPMENT
GO Biological Process (92): angiogenesis (GO:0001525), branching involved in blood vessel morphogenesis (GO:0001569), vasculogenesis (GO:0001570), neural crest cell migration (GO:0001755), neuron migration (GO:0001764), positive regulation of endothelial cell proliferation (GO:0001938), sprouting angiogenesis (GO:0002040), cell migration involved in sprouting angiogenesis (GO:0002042), outflow tract septum morphogenesis (GO:0003148), substrate-dependent cell migration, cell extension (GO:0006930), signal transduction (GO:0007165), integrin-mediated signaling pathway (GO:0007229), cell-cell signaling (GO:0007267), axon guidance (GO:0007411), axonal fasciculation (GO:0007413), motor neuron axon guidance (GO:0008045), response to wounding (GO:0009611), animal organ morphogenesis (GO:0009887), positive regulation of endothelial cell migration (GO:0010595), positive regulation of smooth muscle cell migration (GO:0014911), facial nerve structural organization (GO:0021612), trigeminal nerve structural organization (GO:0021637), vestibulocochlear nerve structural organization (GO:0021649), branchiomotor neuron axon guidance (GO:0021785), gonadotrophin-releasing hormone neuronal migration to the hypothalamus (GO:0021828), regulation of vascular endothelial growth factor receptor signaling pathway (GO:0030947), retinal ganglion cell axon guidance (GO:0031290), regulation of Cdc42 protein signal transduction (GO:0032489), cellular response to hepatocyte growth factor stimulus (GO:0035729), endothelial cell chemotaxis (GO:0035767), cellular response to vascular endothelial growth factor stimulus (GO:0035924), ventral trunk neural crest cell migration (GO:0036486), neuropilin signaling pathway (GO:0038189), VEGF-activated neuropilin signaling pathway (GO:0038190), positive regulation of phosphorylation (GO:0042327), negative regulation of neuron apoptotic process (GO:0043524), positive regulation of angiogenesis (GO:0045766), symbiont entry into host cell (GO:0046718), platelet-derived growth factor receptor signaling pathway (GO:0048008), vascular endothelial growth factor receptor signaling pathway (GO:0048010)
GO Molecular Function (11): vascular endothelial growth factor receptor activity (GO:0005021), GTPase activator activity (GO:0005096), heparin binding (GO:0008201), coreceptor activity (GO:0015026), semaphorin receptor activity (GO:0017154), growth factor binding (GO:0019838), protein kinase binding (GO:0019901), cytokine binding (GO:0019955), vascular endothelial growth factor binding (GO:0038085), metal ion binding (GO:0046872), protein binding (GO:0005515)
GO Cellular Component (19): semaphorin receptor complex (GO:0002116), obsolete extracellular space (GO:0005615), early endosome (GO:0005769), cytosol (GO:0005829), neurofilament (GO:0005883), plasma membrane (GO:0005886), focal adhesion (GO:0005925), axon (GO:0030424), cytoplasmic vesicle (GO:0031410), mitochondrial membrane (GO:0031966), neuron projection (GO:0043005), signaling receptor complex (GO:0043235), postsynaptic membrane (GO:0045211), sorting endosome (GO:0097443), glutamatergic synapse (GO:0098978), extracellular region (GO:0005576), cytoplasm (GO:0005737), mitochondrion (GO:0005739), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-5 pathways:
| Category | Pathways |
|---|---|
| Semaphorin interactions | 3 |
| L1CAM interactions | 2 |
| Signaling by VEGF | 1 |
| Axon guidance | 1 |
| Early SARS-CoV-2 Infection Events | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cytoplasm | 4 |
| cellular anatomical structure | 4 |
| blood vessel morphogenesis | 3 |
| angiogenesis | 2 |
| cell communication | 2 |
| signaling | 2 |
| positive regulation of cell migration | 2 |
| protein binding | 2 |
| endosome | 2 |
| anatomical structure formation involved in morphogenesis | 1 |
| branching morphogenesis of an epithelial tube | 1 |
| cell differentiation | 1 |
| neural crest cell development | 1 |
| mesenchymal cell migration | 1 |
| cell migration | 1 |
| generation of neurons | 1 |
| endothelial cell proliferation | 1 |
| regulation of endothelial cell proliferation | 1 |
| positive regulation of epithelial cell proliferation | 1 |
| sprouting angiogenesis | 1 |
| blood vessel endothelial cell migration | 1 |
| outflow tract morphogenesis | 1 |
| cardiac septum morphogenesis | 1 |
| substrate-dependent cell migration | 1 |
| plasma membrane bounded cell projection assembly | 1 |
| cellular process | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| cell surface receptor signaling pathway | 1 |
| axonogenesis | 1 |
| neuron projection guidance | 1 |
| neuron recognition | 1 |
| axon development | 1 |
| neuron projection fasciculation | 1 |
| axon guidance | 1 |
| response to stress | 1 |
| anatomical structure morphogenesis | 1 |
| animal organ development | 1 |
| regulation of endothelial cell migration | 1 |
| endothelial cell migration | 1 |
Protein interactions and networks
STRING
2336 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| NRP1 | SEMA3A | Q14563 | 999 |
| NRP1 | PLXNA1 | Q9UIW2 | 998 |
| NRP1 | KDR | P35968 | 997 |
| NRP1 | PGF | P49763 | 997 |
| NRP1 | PLXNA4 | Q9HCM2 | 997 |
| NRP1 | VEGFB | P49765 | 996 |
| NRP1 | PLXNA3 | P51805 | 996 |
| NRP1 | SEMA3F | Q13275 | 994 |
| NRP1 | PLXNA2 | O75051 | 992 |
| NRP1 | SEMA3B | Q13214 | 992 |
| NRP1 | GIPC1 | O14908 | 990 |
| NRP1 | FLT1 | P16057 | 990 |
| NRP1 | SEMA3D | O95025 | 986 |
| NRP1 | L1CAM | P32004 | 985 |
| NRP1 | SEMA3C | Q99985 | 979 |
IntAct
109 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| ARRDC1 | WWP2 | psi-mi:“MI:0914”(association) | 0.850 |
| NRP1 | CSNK2A2 | psi-mi:“MI:0914”(association) | 0.790 |
| NRP1 | VEGFA | psi-mi:“MI:0915”(physical association) | 0.770 |
| VEGFA | NRP1 | psi-mi:“MI:0915”(physical association) | 0.770 |
| KDR | NRP1 | psi-mi:“MI:0915”(physical association) | 0.700 |
| S | NRP1 | psi-mi:“MI:0914”(association) | 0.640 |
| NRP1 | S | psi-mi:“MI:0407”(direct interaction) | 0.640 |
| NRP1 | S | psi-mi:“MI:0915”(physical association) | 0.640 |
| CAMKV | AP3B1 | psi-mi:“MI:0914”(association) | 0.640 |
| FLNA | NRP1 | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| NRP1 | FLNA | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| EVA1C | UPK3BL1 | psi-mi:“MI:0914”(association) | 0.530 |
| GPR183 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| TAFA4 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| TMX1 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| FZD10 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| LIPG | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
BioGRID (425): NRP1 (Affinity Capture-MS), PDGFB (Affinity Capture-Western), KDR (Affinity Capture-Western), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-MS), NRP1 (Affinity Capture-Western), NRP1 (Affinity Capture-MS), KCTD9 (Affinity Capture-MS), BCS1L (Affinity Capture-MS)
ESM2 similar proteins: A2AJ76, F1QVU0, O08628, O14786, O88204, O89103, P09529, P0DV84, P15306, P28824, P42917, P79795, P97333, P97793, P97857, Q14393, Q15113, Q501P1, Q53RD9, Q5RBP1, Q60750, Q61398, Q61592, Q61810, Q63772, Q6UXI9, Q80ZD7, Q80ZD8, Q8K099, Q8N441, Q8N8Z6, Q8NDA2, Q8WXS8, Q91V88, Q923P0, Q96NU0, Q9BXP8, Q9BZ76, Q9ESS6, Q9ET61
Diamond homologs: A2AJA7, O14786, P28824, P85171, P98072, P98073, P98157, Q0PMG2, Q0WYX8, Q63191, Q6UXC1, Q8NFP4, Q8QFX6, Q9QWJ9, A2RUV9, A5A6K7, O17754, O18806, O35276, O35375, O35474, O43854, O54858, O54991, O60462, O75976, O88783, O89001, P00451, P02886, P02887, P02888, P04836, P12259, P12263, P14384, P15087, P15169, P16870, P21956
SIGNOR signaling
7 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| DLL4 | “down-regulates quantity by repression” | NRP1 | “transcriptional regulation” |
| NRP1 | “up-regulates quantity by expression” | PHACTR1 | “transcriptional regulation” |
| NRP1 | “form complex” | “CoV2 spike protein-NRP1” | binding |
| SEMA3B | “up-regulates activity” | NRP1 | binding |
| SEMA3A | “up-regulates activity” | NRP1 | binding |
| SEMA3A | down-regulates | NRP1 | binding |
| EMX1 | “up-regulates quantity by expression” | NRP1 | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
326 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 184 |
| Likely benign | 102 |
| Benign | 16 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3137 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 10:33180362:CTCC:C | acceptor_gain | 1.0000 |
| 10:33180363:TCC:T | acceptor_gain | 1.0000 |
| 10:33180364:CC:C | acceptor_gain | 1.0000 |
| 10:33180364:CCCTA:C | acceptor_gain | 1.0000 |
| 10:33180365:CCTA:C | acceptor_gain | 1.0000 |
| 10:33180366:C:A | acceptor_loss | 1.0000 |
| 10:33180366:C:CC | acceptor_gain | 1.0000 |
| 10:33180368:A:C | acceptor_gain | 1.0000 |
| 10:33182758:C:CT | acceptor_gain | 1.0000 |
| 10:33182767:T:TC | acceptor_gain | 1.0000 |
| 10:33185622:ACTT:A | donor_loss | 1.0000 |
| 10:33185623:CT:C | donor_loss | 1.0000 |
| 10:33185624:TT:T | donor_loss | 1.0000 |
| 10:33185625:TA:T | donor_loss | 1.0000 |
| 10:33185626:A:AC | donor_gain | 1.0000 |
| 10:33185626:ACT:A | donor_loss | 1.0000 |
| 10:33185627:C:CC | donor_gain | 1.0000 |
| 10:33185627:C:CG | donor_loss | 1.0000 |
| 10:33192435:G:GC | acceptor_gain | 1.0000 |
| 10:33207567:ATTAC:A | donor_loss | 1.0000 |
| 10:33207568:TTA:T | donor_loss | 1.0000 |
| 10:33207569:TA:T | donor_loss | 1.0000 |
| 10:33207717:C:CC | acceptor_gain | 1.0000 |
| 10:33221864:C:CC | acceptor_gain | 1.0000 |
| 10:33226128:A:C | donor_gain | 1.0000 |
| 10:33226128:ACTT:A | donor_loss | 1.0000 |
| 10:33226129:CTTA:C | donor_loss | 1.0000 |
| 10:33226130:TTACA:T | donor_loss | 1.0000 |
| 10:33226131:T:TG | donor_loss | 1.0000 |
| 10:33226132:A:AC | donor_gain | 1.0000 |
AlphaMissense
6118 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 10:33180253:A:C | S865R | 1.000 |
| 10:33180253:A:T | S865R | 1.000 |
| 10:33180255:T:G | S865R | 1.000 |
| 10:33192324:C:A | W673C | 1.000 |
| 10:33192324:C:G | W673C | 1.000 |
| 10:33192326:A:G | W673R | 1.000 |
| 10:33192326:A:T | W673R | 1.000 |
| 10:33254066:A:G | W315R | 1.000 |
| 10:33254066:A:T | W315R | 1.000 |
| 10:33270704:A:G | F134S | 1.000 |
| 10:33270731:G:A | S125F | 1.000 |
| 10:33330788:C:A | W56C | 1.000 |
| 10:33330788:C:G | W56C | 1.000 |
| 10:33330790:A:G | W56R | 1.000 |
| 10:33330790:A:T | W56R | 1.000 |
| 10:33180234:C:G | G872R | 0.999 |
| 10:33180234:C:T | G872R | 0.999 |
| 10:33180246:C:G | G868R | 0.999 |
| 10:33180246:C:T | G868R | 0.999 |
| 10:33186262:C:A | W763C | 0.999 |
| 10:33186262:C:G | W763C | 0.999 |
| 10:33186421:G:C | S710R | 0.999 |
| 10:33186421:G:T | S710R | 0.999 |
| 10:33186423:T:G | S710R | 0.999 |
| 10:33192354:C:A | W663C | 0.999 |
| 10:33192354:C:G | W663C | 0.999 |
| 10:33207707:C:G | G542R | 0.999 |
| 10:33221787:C:G | R405P | 0.999 |
| 10:33226182:G:C | S363R | 0.999 |
| 10:33226182:G:T | S363R | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000002801 (10:33293342 G>A,T), RS1000016611 (10:33266124 C>T), RS1000025753 (10:33270918 A>C,G), RS1000049792 (10:33322709 A>G), RS1000064905 (10:33266422 G>A), RS1000069820 (10:33227192 T>G), RS1000091315 (10:33200247 G>T), RS1000129222 (10:33260253 T>C), RS1000180194 (10:33179368 T>C), RS1000204366 (10:33177826 C>T), RS1000213983 (10:33280757 A>T), RS1000229961 (10:33260626 G>A), RS1000240008 (10:33304925 A>C), RS1000248330 (10:33319290 G>A), RS1000254019 (10:33298925 C>T)
Disease associations
OMIM: gene MIM:602069 | disease phenotypes:
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| congenital heart disease | Limited | Autosomal recessive |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| congenital heart disease | Limited | AR |
Mondo (1): congenital heart disease (MONDO:0005453)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
19 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001119_1 | Schizophrenia | 6.000000e-06 |
| GCST001807_2 | Tetralogy of Fallot | 2.000000e-07 |
| GCST003720_37 | Migraine | 2.000000e-09 |
| GCST004746_21 | Small cell lung carcinoma | 1.000000e-06 |
| GCST005196_29 | Coronary artery disease | 3.000000e-06 |
| GCST006585_233 | Blood protein levels | 1.000000e-14 |
| GCST006585_917 | Blood protein levels | 3.000000e-25 |
| GCST010241_88 | Apolipoprotein A1 levels | 5.000000e-13 |
| GCST010242_234 | HDL cholesterol levels | 1.000000e-08 |
| GCST010242_37 | HDL cholesterol levels | 2.000000e-15 |
| GCST010396_57 | Gut microbiota (bacterial taxa, hurdle binary method) | 8.000000e-06 |
| GCST010703_186 | Brain morphology (MOSTest) | 6.000000e-11 |
| GCST90002405_257 | Reticulocyte count | 3.000000e-09 |
| GCST90013445_49 | Type 1 diabetes | 3.000000e-15 |
| GCST90013445_59 | Type 1 diabetes | 3.000000e-15 |
| GCST90020025_387 | Waist-to-hip ratio adjusted for BMI | 2.000000e-08 |
| GCST90020025_388 | Waist-to-hip ratio adjusted for BMI | 2.000000e-08 |
| GCST90020027_867 | Waist-hip index | 2.000000e-08 |
| GCST90020027_868 | Waist-hip index | 3.000000e-08 |
EFO canonical traits (6, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004614 | apolipoprotein A 1 measurement |
| EFO:0004612 | high density lipoprotein cholesterol measurement |
| EFO:0007874 | gut microbiome measurement |
| EFO:0004346 | neuroimaging measurement |
| EFO:0007986 | reticulocyte count |
| EFO:0007788 | BMI-adjusted waist-hip ratio |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| 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 (2): CHEMBL5174 (SINGLE PROTEIN), CHEMBL5482974 (PROTEIN-PROTEIN INTERACTION)
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
1 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs2070296 | Efficacy | 3 | ranibizumab | Macular Degeneration |
PharmGKB variants
4 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs2070296 | NRP1 | 3 | 2.25 | 1 | ranibizumab |
| rs2229935 | NRP1 | 0.00 | 0 | ||
| rs2247383 | NRP1 | 0.00 | 0 | ||
| rs2804495 | NRP1 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: other protein — Neuropilins and Plexins
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| EG01377 | Competitive | 5.88 | pKd |
| EG00229 | Competitive | 5.05 | pIC50 |
Binding affinities (BindingDB)
34 measured of 480 human assays (496 total across all organisms); most potent 34 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 2-methoxy-N-(2-morpholinophenyl)-5-(phthalimidomethyl)benzamide | EC50 | 340 nM |
| cid_2467179 | EC50 | 577 nM |
| 4-[(2S)-4-methyl-1-phenoxypentan-2-yl]-1-(2-phenylethyl)-1,4-diazepan-5-one | EC50 | 2690 nM |
| 1,1-bis(oxidanylidene)-2-(phenylmethyl)-3,4-dihydro-1,2-benzothiazepin-5-one | EC50 | 3060 nM |
| 4-[(N-besylanilino)methyl]-N-(2,6-diethylphenyl)benzamide | EC50 | 3430 nM |
| N-(4-hydroxyphenyl)-2-(4-isobutylphenyl)propanamide | EC50 | 3770 nM |
| 4-[(4-methyl-5,6,7,8-tetrahydroquinazolin-2-yl)sulfanylmethyl]benzoic acid | IC50 | 4530 nM |
| cid_2535143 | IC50 | 7370 nM |
| 3-(2-pyridinylamino)-2H-isoquinolin-1-one | IC50 | 7380 nM |
| SMR000120104 | IC50 | 9900 nM |
| cid_3251511 | IC50 | 10600 nM |
| 5-azanyl-3-(4-chlorophenyl)-N-[(E)-(4-methoxyphenyl)methylideneamino]-4-oxidanylidene-thieno[3,4-d]pyridazine-1-carboxamide | IC50 | 11900 nM |
| (1-phenylpyrazolo[3,4-d]pyrimidin-4-yl)diazane | EC50 | 12800 nM |
| SMR000061158 | IC50 | 18900 nM |
| SMR000335434 | IC50 | 19900 nM |
| cid_16193520 | IC50 | 20100 nM |
| 2-[6-hydroxy-5-methyl-1-(4-methylphenyl)-4-oxopyrimidin-2-yl]sulfanyl-N-(3-methoxyphenyl)acetamide | IC50 | 20100 nM |
| cid_665545 | IC50 | 23200 nM |
| MLS000046765 | IC50 | 27700 nM |
| 1-[4-(1-azanyl-2-methyl-propyl)-1,3-thiazol-2-yl]-3-[3-(trifluoromethyl)phenyl]urea | IC50 | 29900 nM |
| (4E)-5-methyl-4-[(3-nitroanilino)methylene]-2-phenyl-2-pyrazoline-3-thione | IC50 | 31100 nM |
| quinolin-8-yl N-[(2,4-dichlorophenyl)amino]-2-oxidanylidene-propanimidothioate | IC50 | 32200 nM |
| 2-(2-methylphenoxy)-N-[(2-methylphenyl)carbamothioyl]ethanamide | IC50 | 33800 nM |
| [4-(4-Chloro-phenyl)-5-(2,4-dichloro-phenyl)-4H-[1,2,4]triazol-3-ylsulfanyl]-acetic acid | IC50 | 34400 nM |
| (6Z)-6-(3-pyrazolin-3-ylidene)cyclohexa-2,4-dien-1-one | IC50 | 35000 nM |
| 4-methyl-N’-(4-methylphenyl)benzenesulfonohydrazide | IC50 | 37900 nM |
| SMR000127729 | IC50 | 38000 nM |
| ethyl 2-(1,3-benzodioxol-5-ylamino)ethanoate | IC50 | 38700 nM |
| cid_4557552 | IC50 | 39500 nM |
| cid_4875488 | IC50 | 40100 nM |
| MLS000516671 | IC50 | 40500 nM |
| MLS000554687 | IC50 | 56100 nM |
| 3-chloranyl-5-(3,4-dimethoxyphenyl)-7-(trifluoromethyl)-1,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxylic acid | IC50 | 57500 nM |
| MLS000031979 | IC50 | 75600 nM |
ChEMBL bioactivities
119 potent at pChembl≥5 of 191 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.22 | IC50 | 0.598 | nM | CHEMBL5557974 |
| 7.87 | Kd | 13.4 | nM | CHEMBL5591272 |
| 7.75 | Kd | 17.6 | nM | CHEMBL5594653 |
| 7.65 | Kd | 22.5 | nM | CHEMBL5575279 |
| 7.41 | IC50 | 39 | nM | CHEMBL5398256 |
| 7.37 | IC50 | 43.05 | nM | CHEMBL5398256 |
| 7.34 | IC50 | 46 | nM | CHEMBL5421065 |
| 7.33 | IC50 | 46.24 | nM | CHEMBL5421065 |
| 7.12 | Kd | 76 | nM | CHEMBL4207210 |
| 7.12 | Kd | 76.3 | nM | CHEMBL5570585 |
| 7.01 | Kd | 96.7 | nM | CHEMBL5572893 |
| 6.98 | Kd | 105.6 | nM | CHEMBL5574160 |
| 6.48 | IC50 | 330 | nM | CHEMBL5424756 |
| 6.48 | IC50 | 328.9 | nM | CHEMBL5424756 |
| 6.39 | Kd | 410 | nM | CHEMBL4205347 |
| 6.36 | IC50 | 440 | nM | CHEMBL5430767 |
| 6.36 | IC50 | 434.5 | nM | CHEMBL5430767 |
| 6.21 | IC50 | 609 | nM | CHEMBL4217624 |
| 6.20 | IC50 | 630 | nM | CHEMBL5436656 |
| 6.20 | IC50 | 626.6 | nM | CHEMBL5436656 |
| 6.17 | Kd | 680 | nM | CHEMBL4208692 |
| 6.16 | IC50 | 700 | nM | CHEMBL5420922 |
| 6.16 | IC50 | 698.2 | nM | CHEMBL5420922 |
| 6.10 | IC50 | 800 | nM | CHEMBL4279036 |
| 6.09 | IC50 | 810 | nM | CHEMBL5437088 |
| 6.09 | IC50 | 811 | nM | CHEMBL5437088 |
| 6.08 | Kd | 840 | nM | CHEMBL4204363 |
| 6.05 | IC50 | 890 | nM | CHEMBL5427459 |
| 6.05 | IC50 | 891.2 | nM | CHEMBL5427459 |
| 5.95 | IC50 | 1130 | nM | CHEMBL5409821 |
| 5.95 | IC50 | 1122 | nM | CHEMBL5409821 |
| 5.93 | Kd | 1170 | nM | CHEMBL4207015 |
| 5.88 | Kd | 1330 | nM | CHEMBL4202667 |
| 5.88 | Kd | 1320 | nM | CHEMBL4217624 |
| 5.88 | IC50 | 1330 | nM | CHEMBL5413708 |
| 5.88 | IC50 | 1318 | nM | CHEMBL5413708 |
| 5.86 | Kd | 1380 | nM | CHEMBL4209931 |
| 5.85 | Kd | 1410 | nM | CHEMBL4214846 |
| 5.84 | Kd | 1450 | nM | CHEMBL4216033 |
| 5.84 | Kd | 1430 | nM | CHEMBL4204935 |
| 5.82 | Kd | 1500 | nM | CHEMBL4211378 |
| 5.81 | Kd | 1560 | nM | CHEMBL4214327 |
| 5.81 | IC50 | 1540 | nM | CHEMBL5432970 |
| 5.81 | IC50 | 1549 | nM | CHEMBL5432970 |
| 5.80 | IC50 | 1600 | nM | CHEMBL4217624 |
| 5.75 | Kd | 1770 | nM | CHEMBL4212550 |
| 5.73 | Kd | 1860 | nM | CHEMBL4218751 |
| 5.73 | Kd | 1870 | nM | CHEMBL4213216 |
| 5.70 | IC50 | 2000 | nM | CHEMBL387002 |
| 5.70 | IC50 | 2000 | nM | CHEMBL215821 |
PubChem BioAssay actives
118 with measured affinity, of 475 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 |
|---|---|---|---|---|
| 2-anilino-4-(4-methyl-2-morpholin-4-ylpyrimidin-5-yl)-1H-pyrimidin-6-one | 2066984: Inhibition of [125I]-VEGF-A165 binding to NRP1 (unknown origin) in HUVEC cells | ic50 | 0.0006 | uM |
| (4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3R)-2-[[(3S,6S,9S,12S,15S,21S,24R,29R,32S,35S,38S,41S)-24-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-32-(4-aminobutyl)-3,35-dibenzyl-9-(3-carbamimidamidopropyl)-21-(hydroxymethyl)-6-[(4-hydroxyphenyl)methyl]-38-(1H-indol-3-ylmethyl)-12-(2-methylpropyl)-2,5,8,11,14,20,23,31,34,37,40-undecaoxo-26,27-dithia-1,4,7,10,13,19,22,30,33,36,39-undecazatricyclo[39.3.0.015,19]tetratetracontane-29-carbonyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[2-[[2-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.0134 | uM |
| (4S)-4-[[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S,3R)-2-[[(3S,9S,12S,15S,21S,24R,29R,32S,35S,38S,41S)-24-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-9,21-bis(3-carbamimidamidopropyl)-3-(carboxymethyl)-35,38-bis(1H-indol-3-ylmethyl)-32-methyl-2,5,8,11,14,20,23,31,34,37,40-undecaoxo-12-propan-2-yl-26,27-dithia-1,4,7,10,13,19,22,30,33,36,39-undecazatricyclo[39.3.0.015,19]tetratetracontane-29-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[2-[[2-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.0176 | uM |
| (4S)-4-[[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(3S,6S,9S,12S,15S,21S,24R,29R,32S,35S,38S,41S)-24-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-benzyl-12-[(2S)-butan-2-yl]-9,32-bis(3-carbamimidamidopropyl)-21-(hydroxymethyl)-35,38-bis(1H-indol-3-ylmethyl)-6-(2-methylsulfanylethyl)-2,5,8,11,14,20,23,31,34,37,40-undecaoxo-26,27-dithia-1,4,7,10,13,19,22,30,33,36,39-undecazatricyclo[39.3.0.015,19]tetratetracontane-29-carbonyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[2-[[2-[[(2S)-6-amino-1-[[(2S)-1-[(2S)-2-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(1S)-4-carbamimidamido-1-carboxybutyl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.0225 | 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 |
| (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 | 2016516: Inhibition of human biotinylated-VEGFA165 binding to recombinant human NRP-1 measured after 2 hrs by chemiluminescent based ELISA | ic50 | 0.0460 | uM |
| (3S)-4-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-3-[[(1R,4S,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R,40S,43S,46S,49S,52S,55S,58R,65S,68R)-34,55-bis(4-aminobutyl)-13,52-bis(2-amino-2-oxoethyl)-25-(3-amino-3-oxopropyl)-7,28,40,65-tetrakis(3-carbamimidamidopropyl)-10,19-bis(2-carboxyethyl)-46-(carboxymethyl)-4,49-bis[(1R)-1-hydroxyethyl]-43-(hydroxymethyl)-58-[[(2S)-3-hydroxy-2-(octanoylamino)propanoyl]amino]-31-methyl-16,22-bis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51,54,57,63,66-henicosaoxo-60,61,70,71-tetrathia-2,5,8,11,14,17,20,23,26,29,32,35,38,41,44,47,50,53,56,64,67-henicosazabicyclo[35.25.10]doheptacontane-68-carbonyl]amino]-4-oxobutanoic acid | 1369559: Binding affinity to recombinant human NRP1 extracellular domain by SPR method | kd | 0.0760 | uM |
| (4S)-4-[[(2S)-1-[(2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(3S,6S,9S,12S,15S,18S,21R,26R,29S,32S,35S,38S)-21-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-9,18,29-tris(3-carbamimidamidopropyl)-3-(hydroxymethyl)-6-(1H-imidazol-5-ylmethyl)-32,35-bis(1H-indol-3-ylmethyl)-15-methyl-12-(2-methylpropyl)-2,5,8,11,14,17,20,28,31,34,37-undecaoxo-23,24-dithia-1,4,7,10,13,16,19,27,30,33,36-undecazabicyclo[36.3.0]hentetracontane-26-carbonyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[2-[[2-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[(2S)-2-[[(1S)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.0763 | uM |
| (4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(3S,6S,9S,12S,15S,21S,24R,29R,32S,35S,38S,41S)-24-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-carboxypropanoyl]amino]hexanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-3,35-bis(4-aminobutyl)-32-benzyl-12-[(2S)-butan-2-yl]-9-(3-carbamimidamidopropyl)-6-(carboxymethyl)-38-(1H-indol-3-ylmethyl)-21-(2-methylpropyl)-2,5,8,11,14,20,23,31,34,37,40-undecaoxo-26,27-dithia-1,4,7,10,13,19,22,30,33,36,39-undecazatricyclo[39.3.0.015,19]tetratetracontane-29-carbonyl]amino]-4-oxobutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[2-[[2-[[2-[[(2S)-6-amino-1-[[2-[[(2S)-4-amino-1-[[(2S)-5-carbamimidamido-1-[(2S)-2-[(2S)-2-[[(1S)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.0967 | uM |
| (4R)-4-[[2-[[(2R)-2-[[2-[[2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-6-amino-2-[[(2R)-4-carboxy-2-[[(2R)-2-[[2-[[2-[[(2R)-3-(4-hydroxyphenyl)-2-[[(2R)-2-[[2-[[(2R)-3-(4-hydroxyphenyl)-2-[[(2R)-2-[[(2R)-2-[(2-naphthalen-2-ylacetyl)amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]acetyl]amino]acetyl]amino]-4-methylsulfanylbutanoyl]amino]butanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-[[(2R)-5-carbamimidamido-1-[(2R)-2-[(2R)-2-[[(1R)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-5-oxopentanoic acid | 2096070: Binding affinity to NRP1 (unknown origin) by MST analysis | kd | 0.1056 | 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)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-(pyridin-2-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 0.4100 | 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 |
| (2S)-2-[[3-[[5-[4-(aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369537: Inhibition of biotinylated VEGF-A binding to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells after 2 hrs | ic50 | 0.6090 | 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)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-(pyridin-2-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 0.6800 | 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-[4-amino-2-[[2-amino-6-(diaminomethylideneamino)hexanoyl]amino]butanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1421450: Inhibition of biotinylated VEGF165 binding to NRP1 (unknown origin) by ELISA | ic50 | 0.8000 | 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)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-(1H-imidazol-2-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 0.8400 | 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)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-(piperidin-1-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.1700 | 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 |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-[[4-(methylcarbamoyl)piperidin-1-yl]methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.3300 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.3800 | uM |
| (2S)-2-[[3-[[5-[3-[[4-(cyanomethyl)piperidin-1-yl]methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.4100 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-(1H-pyrazol-4-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.4300 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[3-(1H-pyrazol-5-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.4500 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-[(4-morpholin-4-ylpiperidin-1-yl)methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.5000 | uM |
| (2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]-2-[[(2S)-2-amino-3-hydroxypropanoyl]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 | 1.5400 | uM |
| (2S)-2-[[3-[[5-[3-[(4-carbamoylpiperidin-1-yl)methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.5600 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-(1H-imidazol-2-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.7700 | uM |
| (2S)-2-[[3-[[5-[2-[[4-(cyanomethyl)piperidin-1-yl]methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.8600 | uM |
| (2S)-2-[[3-[[5-[2-(aminomethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 1.8700 | uM |
| 5-chloro-2-(3-fluorophenyl)-3-(2-phenylethylamino)indolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| 5-chloro-2-phenyl-3-(2-phenylethylamino)indolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| 5-chloro-2-(2-phenylethyl)-3-(2-phenylethylamino)indolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| 5-chloro-3-(2-phenylethylamino)-2-pyridin-2-ylindolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| 5-chloro-2-(3-methoxyphenyl)-3-(2-phenylethylamino)indolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| 5-chloro-2-(4-chlorophenyl)-3-(2-phenylethylamino)indolizine-1-carbonitrile | 269821: Inhibition of VEGF165-NRP1 interaction by ELISA | ic50 | 2.0000 | uM |
| (2S)-2-[[3-[[5-[2-[(4-carbamoylpiperidin-1-yl)methyl]phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 2.0500 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-(1H-pyrazol-5-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 2.1000 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-(1H-pyrazol-4-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 2.1400 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-(2,3-dihydro-1H-isoindol-5-yl)-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 2.1700 | uM |
| (2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-6-(diaminomethylideneamino)-2-(3-sulfanylpropanoylamino)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 | 2.1700 | uM |
| (2S)-2-[[(2S,3aS,7aS)-1-[(2S)-4-amino-2-[[(2S)-2-amino-6-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]hexanoyl]amino]butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid | 1637868: Inhibition of human biotinylated VEGF-A165 binding to recombinant human NRP1 receptor after 2 hrs by chemiluminescence analysis | ic50 | 2.2387 | uM |
| (2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-amino-4-[[(2S)-2-amino-6-(diaminomethylideneamino)hexanoyl]amino]butanoyl]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 | 2.2387 | uM |
| (2S)-5-(diaminomethylideneamino)-2-[[3-[[5-[2-(piperidin-1-ylmethyl)phenyl]-2,3-dihydro-1-benzofuran-7-yl]sulfonylamino]thiophene-2-carbonyl]amino]pentanoic acid | 1369535: Binding affinity to N-terminal His6-tagged recombinant human NRP1-b1 domain expressed in Escherichia coli Rosetta Gami 2 (DE3) pLysS cells by SPR method | kd | 2.2800 | uM |
| (2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-aminobutanoyl]amino]-6-[[(2S)-2-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 | 2.3988 | uM |
CTD chemical–gene interactions
111 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| trichostatin A | affects cotreatment, increases expression, affects expression | 5 |
| Valproic Acid | affects cotreatment, increases expression, decreases expression | 5 |
| bisphenol A | affects cotreatment, increases expression, affects expression, decreases expression, increases methylation | 4 |
| Benzo(a)pyrene | decreases expression, increases expression | 4 |
| (+)-JQ1 compound | affects cotreatment, decreases expression | 3 |
| Tetrachlorodibenzodioxin | affects expression, increases expression | 3 |
| Tretinoin | decreases expression, increases expression | 3 |
| Cyclosporine | decreases expression, increases expression, affects expression | 3 |
| sodium arsenate | decreases expression, increases abundance, increases expression | 2 |
| arsenite | increases expression, increases methylation, decreases reaction | 2 |
| cobaltous chloride | decreases expression | 2 |
| manganese chloride | decreases expression, increases abundance, increases expression, affects cotreatment | 2 |
| mercuric bromide | increases expression, affects cotreatment | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| belinostat | increases expression, affects cotreatment | 2 |
| Decitabine | affects cotreatment, decreases expression, decreases reaction | 2 |
| Troglitazone | increases expression | 2 |
| Panobinostat | affects cotreatment, increases expression | 2 |
| Acetaminophen | decreases expression | 2 |
| Arsenic | increases expression, affects cotreatment, decreases expression, increases abundance | 2 |
| Cadmium | increases abundance, increases expression, decreases expression, decreases reaction | 2 |
| Copper | affects binding, increases expression | 2 |
| Doxorubicin | affects response to substance, decreases expression | 2 |
| Estradiol | decreases reaction, affects cotreatment, decreases expression, increases expression | 2 |
| Manganese | increases expression, affects cotreatment, decreases expression, increases abundance | 2 |
| Phenylmercuric Acetate | affects cotreatment, increases expression | 2 |
| Quercetin | affects expression, decreases expression | 2 |
| Tobacco Smoke Pollution | affects expression | 2 |
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | decreases expression | 2 |
| Aflatoxin B1 | affects expression, increases expression | 2 |
ChEMBL screening assays
50 unique, capped per target: 50 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1101244 | Binding | Displacement of [125I]VEGF-A from human NRP1 expressed in pig aortic endothelial cells at 100 uM | Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. — J Med Chem |
Cellosaurus cell lines
5 cell lines: 4 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1GN | Abcam A-549 NRP1 KO | Cancer cell line | Male |
| CVCL_D7W5 | Ubigene A-549 NRP1 KO | Cancer cell line | Male |
| CVCL_TB09 | HAP1 NRP1 (-) 1 | Cancer cell line | Male |
| CVCL_UE43 | 293T human NRP1 | Transformed cell line | Female |
| CVCL_XR14 | HAP1 NRP1 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
300 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 |
| 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 |
| NCT00115375 | PHASE2 | COMPLETED | Platelet Aggregation Inhibition in Children on Clopidogrel (PICOLO) |
| NCT00350220 | PHASE2 | COMPLETED | Transfusion Strategies in Pediatric Cardiothoracic Surgery |
| NCT00374088 | PHASE2 | COMPLETED | N-Acetylcysteine in Neonatal Congenital Heart Surgery (INACT Study) |
| NCT00538785 | PHASE2 | COMPLETED | A Study to Evaluate MEDI-524 In Children With Hemodynamically Significant Congenital Heart Disease |
| NCT00770705 | PHASE2 | WITHDRAWN | Parenteral Phenoxybenzamine During Congenital Heart Disease Surgery |
| NCT00919945 | PHASE2 | TERMINATED | Impact of Early Enteral Feeding on Splanchnic Blood Flow After Surgery for Critical Heart Disease in the Newborn |
| NCT01063712 | PHASE2 | COMPLETED | Safety and Effectiveness of the Device Nit-Occlud® PDA-R |
| NCT01069510 | PHASE2 | COMPLETED | Spironolactone in Adult Congenital Heart Disease |
| NCT01189981 | PHASE2 | COMPLETED | Effect of eHealth Encouragements to Intensive Exercise in Adolescents With Congenital Heart Disease |
| NCT01330433 | PHASE2 | COMPLETED | Effects of CoSeal on Bleeding & Adhesions in Pediatric Heart Surgery |
| NCT01662037 | PHASE2 | COMPLETED | Bosentan Therapy in Children With Functional Single Ventricle |
| NCT01668264 | PHASE2 | UNKNOWN | Imaging Assessment of Diastolic Function |
| NCT01827059 | PHASE2 | UNKNOWN | Bosentan In Exercise Induced Pulmonary Arterial Hypertension in CongenitaL Heart diseasE |
Related Atlas pages
- Associated diseases: congenital heart disease
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): congenital heart disease