FGF2

gene
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Summary

FGF2 (fibroblast growth factor 2, HGNC:3676) is a protein-coding gene on chromosome 4q28.1, encoding Fibroblast growth factor 2 (P09038). Acts as a ligand for FGFR1, FGFR2, FGFR3 and FGFR4.

The protein encoded by this gene is a member of the fibroblast growth factor (FGF) family. FGF family members bind heparin and possess broad mitogenic and angiogenic activities. This protein has been implicated in diverse biological processes, such as limb and nervous system development, wound healing, and tumor growth. The mRNA for this gene contains multiple polyadenylation sites, and is alternatively translated from non-AUG (CUG) and AUG initiation codons, resulting in five different isoforms with distinct properties. The CUG-initiated isoforms are localized in the nucleus and are responsible for the intracrine effect, whereas, the AUG-initiated form is mostly cytosolic and is responsible for the paracrine and autocrine effects of this FGF.

Source: NCBI Gene 2247 — RefSeq curated summary.

At a glance

  • GWAS associations: 11
  • Clinical variants (ClinVar): 68 total — 1 likely-pathogenic
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • Transcription factor: yes — 10 downstream targets (CollecTRI)
  • MANE Select transcript: NM_001361665

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:3676
Approved symbolFGF2
Namefibroblast growth factor 2
Location4q28.1
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000138685
Ensembl biotypeprotein_coding
OMIM134920
Entrez2247

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000264498, ENST00000608478, ENST00000644866

RefSeq mRNA: 2 — MANE Select: NM_001361665 NM_001361665, NM_002006

CCDS: CCDS34059, CCDS93618

Canonical transcript exons

ENST00000644866 — 3 exons

ExonStartEnd
ENSE00000970285122876321122876424
ENSE00001081614122892211122898236
ENSE00003705888122826831122827352

Expression profiles

Bgee: expression breadth ubiquitous, 232 present calls, max score 93.75.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 39.3252 / max 699.6091, expressed in 1270 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
4954638.42421259
495470.4712260
495450.4297252

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
cartilage tissueUBERON:000241893.75gold quality
choroid plexus epitheliumUBERON:000391193.21gold quality
calcaneal tendonUBERON:000370189.14gold quality
smooth muscle tissueUBERON:000113586.26gold quality
stromal cell of endometriumCL:000225585.92gold quality
descending thoracic aortaUBERON:000234585.77gold quality
adipose tissueUBERON:000101384.82gold quality
pigmented layer of retinaUBERON:000178284.66gold quality
subcutaneous adipose tissueUBERON:000219084.07gold quality
connective tissueUBERON:000238484.03gold quality
thoracic aortaUBERON:000151583.75gold quality
muscle layer of sigmoid colonUBERON:003580583.74gold quality
ascending aortaUBERON:000149683.65gold quality
aortaUBERON:000094782.88gold quality
right coronary arteryUBERON:000162582.79gold quality
islet of LangerhansUBERON:000000682.41gold quality
body of uterusUBERON:000985382.39gold quality
popliteal arteryUBERON:000225082.36gold quality
tibial arteryUBERON:000761082.35gold quality
mucosa of stomachUBERON:000119982.29gold quality
caudate nucleusUBERON:000187382.23gold quality
ventricular zoneUBERON:000305382.08gold quality
lower esophagus muscularis layerUBERON:003583381.77gold quality
esophagogastric junction muscularis propriaUBERON:003584181.72gold quality
lower esophagusUBERON:001347381.68gold quality
tibial nerveUBERON:000132381.46gold quality
adipose tissue of abdominal regionUBERON:000780881.45gold quality
left coronary arteryUBERON:000162681.31gold quality
amygdalaUBERON:000187681.31gold quality
omental fat padUBERON:001041480.98gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 4.

ExperimentMarker?Max mean expression
E-MTAB-7249yes18882.71
E-MTAB-8559yes945.99
E-MTAB-7052yes571.63
E-ANND-3yes4.49
E-CURD-10no263.65
E-MTAB-6142no19.17

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

10 targets.

TargetRegulation
ALPLRepression
ANKHActivation
BMP2Activation
ENPP1Activation
FGFR1Repression
GPC1Repression
HBA1Repression
HBBRepression
MMP13Activation
TGFB1Activation

Upstream regulators (CollecTRI, top): AP1, APLN, AR, ATF4, BMP4, CREB1, CREB3L1, DBP, DLX4, DLX5, E2F3, EGR1, EGR2, EIF2AK3, EPAS1, ERG, ESR1, ETS2, ETV3, FOS, FOSL1, FOSL2, FOXF1, GATA4, HDAC5, HHEX, HIF1A, HLF, HOXA10, HOXA9, HOXB7, HOXB9, ID1, ID3, JUN, KMT2A, LMO2, MBD1, MYB, MYBL2

miRNA regulators (miRDB)

219 targeting FGF2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-6867-5P100.0082.213464
HSA-MIR-5692A100.0074.406850
HSA-MIR-340-5P100.0072.504437
HSA-MIR-450A-1-3P100.0069.331837
HSA-MIR-126-5P100.0072.713180
HSA-MIR-3120-5P100.0065.56965
HSA-MIR-3646100.0073.565283
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-4795-3P100.0074.624024
HSA-LET-7A-3P100.0074.033932
HSA-LET-7B-3P100.0074.083913
HSA-LET-7F-1-3P100.0074.023928
HSA-MIR-98-3P100.0074.083907
HSA-MIR-432-3P100.0067.86705
HSA-MIR-4510100.0066.602050
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-318599.9968.121959
HSA-MIR-186-5P99.9970.833707
HSA-MIR-223-3P99.9970.141140
HSA-MIR-511-3P99.9968.851467
HSA-MIR-428299.9975.366408
HSA-MIR-103A-3P99.9869.141595
HSA-MIR-10799.9869.141595
HSA-MIR-4650-5P99.9864.69999
HSA-MIR-56899.9869.862084
HSA-MIR-499A-5P99.9870.791323
HSA-MIR-480399.9871.993117
HSA-MIR-25-3P99.9874.601817
HSA-MIR-363-3P99.9874.721821

Literature-anchored findings (GeneRIF, showing 40)

  • Significant association with poor survival by bFGF. (PMID:11742492)
  • Snake venom disintegrin significantly suppresses basic fibroblast growth factor-induced human umbilical vein endothelial cell proliferation, but has little effect on normal growth of the cell. (PMID:11864711)
  • Expression of basic fibroblast growth factor (bFGF) was significantly associated with increased microvessel density in cutaneous melanomas (PMID:11891198)
  • b-FGF serum levels were significantly higher in patients with chronic myeloproliferative disorders. (PMID:11891801)
  • bFGF up-regulated UPA in both normal and dystrophic myoblasts. (PMID:11928807)
  • Phosphorylation of STAT-3 in response to basic fibroblast growth factor occurs through a mechanism involving platelet-activating factor, JAK-2, and Src in human umbilical vein endothelial cells (PMID:11940567)
  • Phorbol esters inhibit fibroblast growth factor-2-stimulated fibroblast proliferation by a p38 MAP kinase dependent pathway (PMID:11960370)
  • HTLV-I-transformed T cells, but not HTLV-I-negative CD4(+) T cells, secrete biologically active forms of VEGF and bFGF and induce angiogenesis in vitro. (PMID:11964307)
  • stress-induced release from endothelial cells mediated by integrin alpha v beta 3 (PMID:11976347)
  • plasma basic fibroblast growth factor may have a role in progression of multiple myleoma (PMID:11985797)
  • level spontaneously secreted by patient CLL B-cells quantified; consistently secreted in all patient samples. (PMID:11986954)
  • REVIEW: Association of expression of bFGF with clinical characteristics in human leukemia and lymphoma (PMID:11999550)
  • FGF2 binds to heparin-derived oligosaccharides and stimulates phosphorylation of p42/44 mitogen-activated protein kinase and proliferation of rat mammary fibroblasts. (PMID:12000311)
  • Basic fibroblast growth factor may control proteolysis and fibrinolysis in vessel walls by inducing plasminogen activator inhibitor-1 expression in vascular endothelium. (PMID:12006402)
  • possible role of fibroblast growth factors in expression of genes of the plasminogen activator system in breast fibroblasts (PMID:12008951)
  • role for farnesyl pyrophosphate synthase in fibroblast growth factor-mediated signal transduction (PMID:12020352)
  • Biological activity of substrate-bound basic fibroblast growth factor (FGF2): recruitment of FGF receptor-1 in endothelial cell adhesion contacts (PMID:12032827)
  • FGF-2 and TPA induce matrix metalloproteinase-9 secretion in MCF-7 cells through PKC activation of the Ras/ERK pathway. (PMID:12054499)
  • bFGF and aFGF may suppress endothelial-dependent monocyte recruitment and thus have an anti-inflammatory action during angiogenesis in chronic inflammation but inhibit the immunoinflammatory tumor defense mechanism (PMID:12057924)
  • Noninvasive dynamic fluorescence imaging of human melanomas reveals that targeted inhibition of bFGF or FGFR-1 in melanoma cells blocks tumor growth by apoptosis. (PMID:12080186)
  • expression associated with poor outcome in non-Hodgkin lymphoma (PMID:12087465)
  • FGF2 has a role in controlling normal and premature cranial ossification in humans [review] (PMID:12168799)
  • results show that Hensen’s node and FGFs induce ectopic expression of cardiac lineage markers, and that FGF and TGFbeta family members can modulate early development of the heart (PMID:12172783)
  • Serum levels of angiogenin, basic fibroblast growth factor and endostatin in patients receiving intensive chemotherapy for acute myelogenous leukemia. (PMID:12209593)
  • FGF-2 is a novel modulator of Lef/Tcf-beta-catenin signaling in endothelial cells (PMID:12235165)
  • BFGF may sensitively regulate local bone resorption and remodeling through direct and indirect mechanisms that promote angiogenesis and OC recruitment, formation, differentiation, and activated bone pit resorption. (PMID:12369790)
  • This protein has a modulating control of the differentiation of human osteosarcoma cells. (PMID:12393937)
  • Data show that FGF/FGFR signaling stimulates the DNA-binding and transcriptional activities of Runx2 as well as its expression, and these are largely regulated by the PKC pathway. (PMID:12403780)
  • FGF2 and VEGF release by platelets support cell survival and cell growth of vascular endothelium cells in coculture. (PMID:12428103)
  • FGF2 is inhibited by glypican 3 in hepatocellular carcinoma cells (PMID:12478660)
  • EphA2 does not inhibit endothelial cell survival, migration, sprouting, and corneal angiogenesis induced by this protein. (PMID:12496364)
  • The determination of bFGF will be helpful in estimating the size of infarct lesion at acute stage of cerebral infarction. (PMID:12509902)
  • Paracrine interactions of basic fibroblast growth factor and interleukin-6 in multiple myeloma (PMID:12517814)
  • bFGF has a stimulating role in lymphangiogenesis (PMID:12538477)
  • umbilical cords of 10 control and 10 pre-eclamptic newborns demonstrated that both the umbilical cord arterial wall and Wharton’s jelly contain FGF mainly in complexes with the components of different molecular mass (PMID:12545206)
  • Fibroblast growth factor-2-induced signaling is mediated through lipid raft-associated fibroblast growth factor receptor substrate 2 (PMID:12571252)
  • IL-6r and TNF-alpha increase in parallel to VEGF and FGF-2 with increasing stage of multiple myeloma. (PMID:12574959)
  • VEGF, but not bFGF, was associated with higher tumor grading of NHL and high-grade transformation of low-grade lymphoma. (PMID:12607599)
  • reduction of neointimal hyperplasia was observed in autologous vein grafts treated by Sendai virus human-fibroblast growth factor 2; these grafts demonstrated significant restoration of endothelium-dependent vasorelaxation (PMID:12623787)
  • IL-1beta, TNF-alpha, TGF-beta, and bFGF are involved in bone remodeling regulation, acting as local effectors, possibly under the control of PTH. (PMID:12631070)

Cross-species orthologs

2 orthologs

OrganismSymbolGene ID
mus_musculusFgf2ENSMUSG00000037225
rattus_norvegicusFgf2ENSRNOG00000017392

Paralogs (21): FGF10 (ENSG00000070193), FGF22 (ENSG00000070388), FGF4 (ENSG00000075388), FGF20 (ENSG00000078579), FGF14 (ENSG00000102466), FGF9 (ENSG00000102678), FGF21 (ENSG00000105550), FGF8 (ENSG00000107831), FGF6 (ENSG00000111241), FGF1 (ENSG00000113578), FGF12 (ENSG00000114279), FGF23 (ENSG00000118972), FGF13 (ENSG00000129682), FGF5 (ENSG00000138675), FGF7 (ENSG00000140285), FGF18 (ENSG00000156427), FGF17 (ENSG00000158815), FGF11 (ENSG00000161958), FGF19 (ENSG00000162344), FGF3 (ENSG00000186895), FGF16 (ENSG00000196468)

Protein

Protein identifiers

Fibroblast growth factor 2P09038 (reviewed: P09038)

Alternative names: Basic fibroblast growth factor, Heparin-binding growth factor 2

All UniProt accessions (3): P09038, A0A0A0MQV6, D9ZGF5

UniProt curated annotations — full annotation on UniProt →

Function. Acts as a ligand for FGFR1, FGFR2, FGFR3 and FGFR4. Also acts as an integrin ligand which is required for FGF2 signaling. Binds to integrin ITGAV:ITGB3. Plays an important role in the regulation of cell survival, cell division, cell differentiation and cell migration. Functions as a potent mitogen in vitro. Can induce angiogenesis. Mediates phosphorylation of ERK1/2 and thereby promotes retinal lens fiber differentiation.

Subunit / interactions. Monomer. Homodimer. Interacts with FGFR1, FGFR2, FGFR3 and FGFR4. Affinity between fibroblast growth factors (FGFs) and their receptors is increased by heparan sulfate glycosaminoglycans that function as coreceptors. Interacts with CSPG4, FGFBP1 and TEC. Found in a complex with FGFBP1, FGF1 and FGF2. Interacts with FGFBP3. Interacts with integrin ITGAV:ITGB3; the interaction is required for FGF2 signaling. Interacts with SNORC (via the extracellular domain). Interacts with glypican GPC3.

Subcellular location. Secreted. Nucleus.

Tissue specificity. Expressed in granulosa and cumulus cells. Expressed in hepatocellular carcinoma cells, but not in non-cancerous liver tissue.

Post-translational modifications. Phosphorylation at Tyr-215 regulates FGF2 unconventional secretion. Several N-termini starting at positions 94, 125, 126, 132, 143 and 162 have been identified by direct sequencing.

Miscellaneous. This protein binds heparin more strongly than does aFGF. Starts at an alternative CUG codon. Starts at an alternative CUG codon. Starts at an alternative CUG codon.

Similarity. Belongs to the heparin-binding growth factors family.

Isoforms (4)

UniProt IDNamesCanonical?
P09038-41yes
P09038-12
P09038-23
P09038-34

RefSeq proteins (2): NP_001348594, NP_001997 (=MANE)

Domains & families (InterPro)

IDNameType
IPR002209Fibroblast_GF_famFamily
IPR008996IL1/FGFHomologous_superfamily

Pfam: PF00167

UniProt features (57 total): strand 15, modified residue 7, splice variant 5, mutagenesis site 5, helix 5, site 3, sequence conflict 3, turn 3, compositionally biased region 3, region of interest 2, short sequence motif 2, propeptide 1, chain 1, cross-link 1, binding site 1

Structure

Experimental structures (PDB)

25 structures.

PDBMethodResolution (Å)
8OM6X-RAY DIFFRACTION1.31
8HU7X-RAY DIFFRACTION1.4
8HUEX-RAY DIFFRACTION1.48
4OEEX-RAY DIFFRACTION1.5
1BFGX-RAY DIFFRACTION1.6
4FGFX-RAY DIFFRACTION1.6
4OEGX-RAY DIFFRACTION1.6
2FGFX-RAY DIFFRACTION1.77
4OEFX-RAY DIFFRACTION1.8
1BASX-RAY DIFFRACTION1.9
1BFBX-RAY DIFFRACTION1.9
5X1OX-RAY DIFFRACTION1.9
1BFFX-RAY DIFFRACTION2
1BFCX-RAY DIFFRACTION2.2
1EV2X-RAY DIFFRACTION2.2
1FGAX-RAY DIFFRACTION2.2
1IILX-RAY DIFFRACTION2.3
2BFHX-RAY DIFFRACTION2.5
6L4OX-RAY DIFFRACTION2.6
1II4X-RAY DIFFRACTION2.7
1CVSX-RAY DIFFRACTION2.8
1FQ9X-RAY DIFFRACTION3
1BLASOLUTION NMR
1BLDSOLUTION NMR
2M49SOLUTION NMR

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P09038-F172.180.47

Functional residue map

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

Catalytic / active sites (3): 261 (important for interaction with integrin); 262 (important for interaction with integrin); 267 (important for interaction with integrin)

Ligand- & substrate-binding residues (1): 169

Post-translational modifications (8): 108, 108, 110, 110, 112, 112, 215, 228

Mutagenesis-validated functional residues (5):

PositionPhenotype
181no effect on integrin binding.
186no effect on integrin binding.
188no effect on integrin binding.
261–262abolishes binding to integrin itgav:itgb3 and suppresses fgf2 signaling with loss of erk1/2 activation and reduced abili
267reduces binding to integrin itgav:itgb3 and suppresses fgf2 signaling with reduced erk1/2 activation and reduced ability

Function

Pathways and Gene Ontology

Reactome pathways

48 pathways

IDPathway
R-HSA-109704PI3K Cascade
R-HSA-1257604PIP3 activates AKT signaling
R-HSA-1839122Signaling by activated point mutants of FGFR1
R-HSA-1839130Signaling by activated point mutants of FGFR3
R-HSA-190322FGFR4 ligand binding and activation
R-HSA-190370FGFR1b ligand binding and activation
R-HSA-190372FGFR3c ligand binding and activation
R-HSA-190373FGFR1c ligand binding and activation
R-HSA-190375FGFR2c ligand binding and activation
R-HSA-190377FGFR2b ligand binding and activation
R-HSA-2033519Activated point mutants of FGFR2
R-HSA-2219530Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-2892247POU5F1 (OCT4), SOX2, NANOG activate genes related to proliferation
R-HSA-3000170Syndecan interactions
R-HSA-3000171Non-integrin membrane-ECM interactions
R-HSA-5654219Phospholipase C-mediated cascade: FGFR1
R-HSA-5654221Phospholipase C-mediated cascade; FGFR2
R-HSA-5654227Phospholipase C-mediated cascade; FGFR3
R-HSA-5654228Phospholipase C-mediated cascade; FGFR4
R-HSA-5654687Downstream signaling of activated FGFR1
R-HSA-5654688SHC-mediated cascade:FGFR1
R-HSA-5654689PI-3K cascade:FGFR1
R-HSA-5654693FRS-mediated FGFR1 signaling
R-HSA-5654695PI-3K cascade:FGFR2
R-HSA-5654699SHC-mediated cascade:FGFR2
R-HSA-5654700FRS-mediated FGFR2 signaling
R-HSA-5654704SHC-mediated cascade:FGFR3
R-HSA-5654706FRS-mediated FGFR3 signaling
R-HSA-5654710PI-3K cascade:FGFR3
R-HSA-5654712FRS-mediated FGFR4 signaling

MSigDB gene sets: 648 (showing top): GOBP_POSITIVE_REGULATION_OF_EPITHELIAL_CELL_DIFFERENTIATION, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_HINDBRAIN_DEVELOPMENT, REACTOME_SIGNALING_BY_INSULIN_RECEPTOR, GOBP_RESPONSE_TO_ETHANOL, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, GOBP_LENS_FIBER_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, MODULE_516, GOBP_EPITHELIUM_DEVELOPMENT, BROWNE_HCMV_INFECTION_6HR_DN, GOBP_MUSCLE_TISSUE_DEVELOPMENT, ZHAN_MULTIPLE_MYELOMA_PR_DN, GOBP_BEHAVIOR

GO Biological Process (102): osteoblast differentiation (GO:0001649), branching involved in ureteric bud morphogenesis (GO:0001658), organ induction (GO:0001759), endothelial cell proliferation (GO:0001935), positive regulation of endothelial cell proliferation (GO:0001938), cell migration involved in sprouting angiogenesis (GO:0002042), positive regulation of neuroblast proliferation (GO:0002052), transcription by RNA polymerase II (GO:0006366), chemotaxis (GO:0006935), signal transduction (GO:0007165), Ras protein signal transduction (GO:0007265), nervous system development (GO:0007399), neuroblast proliferation (GO:0007405), positive regulation of cell population proliferation (GO:0008284), fibroblast growth factor receptor signaling pathway (GO:0008543), embryo development ending in birth or egg hatching (GO:0009792), animal organ morphogenesis (GO:0009887), glial cell differentiation (GO:0010001), 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 fibroblast migration (GO:0010764), growth factor dependent regulation of skeletal muscle satellite cell proliferation (GO:0014843), substantia nigra development (GO:0021762), cerebellar granule cell precursor proliferation (GO:0021930), positive regulation of cerebellar granule cell precursor proliferation (GO:0021940), neurogenesis (GO:0022008), hyaluronan catabolic process (GO:0030214), lung development (GO:0030324), regulation of cell migration (GO:0030334), paracrine signaling (GO:0038001), negative regulation of fibroblast growth factor receptor signaling pathway (GO:0040037), wound healing (GO:0042060), inner ear auditory receptor cell differentiation (GO:0042491), positive regulation of cell fate specification (GO:0042660), positive regulation of MAP kinase activity (GO:0043406), positive regulation of MAPK cascade (GO:0043410), phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0043491), positive regulation of blood vessel endothelial cell migration (GO:0043536), negative regulation of blood vessel endothelial cell migration (GO:0043537)

GO Molecular Function (11): fibroblast growth factor receptor binding (GO:0005104), cytokine activity (GO:0005125), integrin binding (GO:0005178), growth factor activity (GO:0008083), heparin binding (GO:0008201), chemokine binding (GO:0019956), chemoattractant activity (GO:0042056), identical protein binding (GO:0042802), histone H3K9me2/3 reader activity (GO:0062072), receptor-receptor interaction (GO:0090722), protein binding (GO:0005515)

GO Cellular Component (4): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), nucleus (GO:0005634), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-18 pathways:

CategoryPathways
FGFR1 ligand binding and activation2
FGFR2 ligand binding and activation2
IRS-mediated signalling1
Intracellular signaling by second messengers1
FGFR1 mutant receptor activation1
FGFR3 mutant receptor activation1
Signaling by FGFR41
FGFR3 ligand binding and activation1
FGFR2 mutant receptor activation1
PI3K/AKT Signaling in Cancer1
Transcriptional regulation of pluripotent stem cells1
Non-integrin membrane-ECM interactions1
Extracellular matrix organization1
Downstream signaling of activated FGFR11
Downstream signaling of activated FGFR21

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
receptor ligand activity3
cell differentiation2
signaling receptor binding2
cellular anatomical structure2
ossification1
branching morphogenesis of an epithelial tube1
ureteric bud morphogenesis1
regulation of animal organ formation1
specification of animal organ identity1
developmental induction1
positive regulation of animal organ morphogenesis1
epithelial cell proliferation1
endothelial cell proliferation1
regulation of endothelial cell proliferation1
positive regulation of epithelial cell proliferation1
sprouting angiogenesis1
blood vessel endothelial cell migration1
neuroblast proliferation1
positive regulation of neurogenesis1
regulation of neuroblast proliferation1
positive regulation of neural precursor cell proliferation1
DNA-templated transcription1
response to chemical1
taxis1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
small GTPase-mediated signal transduction1
system development1
generation of neurons1
neural precursor cell proliferation1
cell population proliferation1
regulation of cell population proliferation1
positive regulation of cellular process1
cell surface receptor protein tyrosine kinase signaling pathway1
cellular response to fibroblast growth factor stimulus1
embryo development1
anatomical structure morphogenesis1

Protein interactions and networks

STRING

5516 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
FGF2FGFR1P11362998
FGF2FGFR2P18443997
FGF2FGFR3P22607997
FGF2KDRP35968995
FGF2HSPG2P98160995
FGF2FGFR4P22455993
FGF2CD44P16070991
FGF2SDC1P18827988
FGF2FLT1P16057979
FGF2FGFBP1Q14512977
FGF2TGFB1P01137971
FGF2SDC4P31431971
FGF2CX3CL1P78423970
FGF2EGFP01133969
FGF2CCL11P50877968

IntAct

80 interactions, top by confidence:

ABTypeScore
FGF2FGFR1psi-mi:“MI:0407”(direct interaction)0.910
FGFR1FGF2psi-mi:“MI:0407”(direct interaction)0.910
FGF2PTX3psi-mi:“MI:0407”(direct interaction)0.790
PTX3FGF2psi-mi:“MI:0407”(direct interaction)0.790
FGF2PTX3psi-mi:“MI:0915”(physical association)0.790
FGFR2FGF2psi-mi:“MI:0407”(direct interaction)0.780
FGF2FGFR2psi-mi:“MI:0407”(direct interaction)0.780
SDC2PDPK1psi-mi:“MI:0914”(association)0.640
CAMKVAP3B1psi-mi:“MI:0914”(association)0.640
FGFBP1FGF2psi-mi:“MI:0407”(direct interaction)0.620

BioGRID (105): FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Protein-peptide), FGF2 (Protein-peptide), FGFR1 (Affinity Capture-Western), PRKACA (Affinity Capture-Western), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-MS), FGF2 (Affinity Capture-Western), FGF2 (Affinity Capture-MS), SDC1 (Co-purification)

ESM2 similar proteins: A0A0U1RR11, A0A0U1RRI6, A6NCS6, A6NJG2, B0BN44, D3YXK1, E9PY61, E9Q0B3, F5H4A9, O00220, O00221, P09038, P0DPI3, P22083, P98077, Q08AU9, Q2M2W7, Q2M3V2, Q2TBI2, Q5F267, Q5FW56, Q5IS69, Q5R866, Q5T4W7, Q5TM52, Q5U4P2, Q5VTJ3, Q659K9, Q673H1, Q69ZB3, Q6AYE8, Q6IPT2, Q6PJ61, Q7RTU4, Q7TSX9, Q7YR31, Q80SU3, Q86SH2, Q86Y97, Q8NBR0

Diamond homologs: A0MTF4, A6P7H6, M3X9S6, O15520, O35565, O43320, O54769, P03968, P03969, P05230, P05524, P08620, P09038, P10767, P11403, P11487, P12034, P12226, P13109, P15655, P15656, P19596, P20002, P20003, P21658, P21781, P31371, P34004, P36363, P36364, P36386, P48798, P48799, P48800, P48801, P48802, P48803, P48804, P48805, P48806

SIGNOR signaling

24 interactions.

AEffectBMechanism
FGF2up-regulatesMAPK14
FGF2up-regulatesRUNX2
FGF2“up-regulates quantity by expression”BMP2“transcriptional regulation”
FGF2up-regulatesFGFR3binding
FGF2“up-regulates quantity by expression”TGFB1“transcriptional regulation”
FGF2up-regulatesMAPK1
FGF2up-regulatesMAPK3
FGF2up-regulatesMAPK8
FGF2up-regulatesFGFR4binding
FGF2“down-regulates quantity by repression”HBB“transcriptional regulation”
FGF2“down-regulates quantity by repression”HBA1“transcriptional regulation”
FGF2“up-regulates quantity by expression”ENPP1“transcriptional regulation”
FGF2“up-regulates quantity by expression”ANKH“transcriptional regulation”
FGF2“down-regulates quantity by repression”ALPL“transcriptional regulation”
FGF2“up-regulates quantity by expression”MMP13“transcriptional regulation”
TP53“down-regulates quantity by repression”FGF2“transcriptional regulation”
HOXB7“up-regulates quantity by expression”FGF2“transcriptional regulation”
FGF2up-regulatesGbeta
FGF2up-regulatesERK1/2
FGF2up-regulatesFGFR2binding
FGF2up-regulatesAngiogenesis

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 43 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.

Reactome pathways:

PathwayPartnersFoldFDR
Defective B4GALT7 causes EDS, progeroid type7117.6×9e-12
Defective B3GAT3 causes JDSSDHD7117.6×9e-12
Defective B3GALT6 causes EDSP2 and SEMDJL17117.6×9e-12
Attachment and Entry6106.1×6e-10
HS-GAG degradation687.6×2e-09
Respiratory syncytial virus (RSV) attachment and entry687.6×2e-09
Initiation of coagulation cascade684.0×2e-09
Glycosaminoglycan-protein linkage region biosynthesis781.1×9e-11

GO biological processes:

GO termPartnersFoldFDR
fibroblast growth factor receptor signaling pathway535.7×4e-05
cell migration913.8×6e-06
positive regulation of ERK1 and ERK2 cascade510.6×6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic1
Uncertain significance49
Likely benign7
Benign2

Top pathogenic / likely-pathogenic (1)

Variant IDHGVSClassification
635942Single alleleLikely pathogenic

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

999 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
4:122827269:T:AL165Q1.000
4:122827269:T:CL165P1.000
4:122827274:T:CC167R1.000
4:122827275:G:AC167Y1.000
4:122827276:C:GC167W1.000
4:122827284:G:AG170E1.000
4:122827292:T:CF173L1.000
4:122827294:C:AF173L1.000
4:122827294:C:GF173L1.000
4:122827325:G:TG184W1.000
4:122827326:G:AG184E1.000
4:122876327:T:CL195P1.000
4:122876363:T:AI207N1.000
4:122876363:T:CI207T1.000
4:122876363:T:GI207S1.000
4:122876368:G:AG209R1.000
4:122876368:G:CG209R1.000
4:122876390:T:CL216P1.000
4:122876408:G:AG222E1.000
4:122876408:G:TG222V1.000
4:122892236:T:CF236S1.000
4:122892243:A:CE238D1.000
4:122892243:A:TE238D1.000
4:122892267:T:AN246K1.000
4:122892267:T:GN246K1.000
4:122892271:T:CY248H1.000
4:122892271:T:GY248D1.000
4:122892305:C:AA259E1.000
4:122892319:G:TG264W1.000
4:122892320:G:AG264E1.000

dbSNP variants (sampled 300 via entrez): RS1000030503 (4:122852159 A>G), RS1000067543 (4:122890089 G>A), RS10000779 (4:122864959 A>C,G,T), RS1000102611 (4:122868247 C>G), RS1000146289 (4:122852431 C>G), RS1000282704 (4:122846083 G>T), RS1000299804 (4:122894792 A>T), RS1000301647 (4:122865672 A>G), RS1000316706 (4:122863919 A>C), RS1000333432 (4:122887836 T>C,G), RS1000438510 (4:122865964 G>C), RS1000444613 (4:122839032 G>A), RS1000489696 (4:122857364 C>T), RS1000502620 (4:122855582 G>C), RS1000514172 (4:122827058 G>A)

Disease associations

OMIM: gene MIM:134920 | disease phenotypes:

GenCC curated gene-disease

Mondo (2): long QT syndrome (MONDO:0002442), neurodevelopmental disorder (MONDO:0700092)

Orphanet (0):

HPO phenotypes

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

GWAS associations

11 associations (top):

StudyTraitp-value
GCST002436_2Irritable bowel syndrome8.000000e-08
GCST002782_12Waist-to-hip ratio adjusted for body mass index3.000000e-07
GCST002782_13Waist-to-hip ratio adjusted for body mass index4.000000e-08
GCST002782_14Waist-to-hip ratio adjusted for body mass index5.000000e-06
GCST002782_15Waist-to-hip ratio adjusted for body mass index3.000000e-07
GCST002783_80Body mass index7.000000e-07
GCST004505_109Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)8.000000e-06
GCST004863_136Mosquito bite size4.000000e-08
GCST007234_10Acne (severe)2.000000e-09
GCST90020024_683A body shape index5.000000e-09
GCST90020025_614Waist-to-hip ratio adjusted for BMI5.000000e-08

EFO canonical traits (5, from GWAS)

EFO IDTrait name
EFO:0007788BMI-adjusted waist-hip ratio
EFO:0004340body mass index
EFO:0004318smoking behavior
EFO:0008378mosquito bite reaction size measurement
EFO:0007789BMI-adjusted waist circumference

MeSH disease descriptors (2)

DescriptorNameTree numbers
D008133Long QT SyndromeC14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547
D065886Neurodevelopmental DisordersF03.625

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3107 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 77 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL3686884E-7090277

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

Binding affinities (BindingDB)

37 measured of 37 human assays (37 total across all organisms); most potent 37 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
Linked sulfated tetracyclitol, 12KD0.4 nM
5-[[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]-4-pyridinyl]oxy]-6-(2-methoxyethoxy)-N-methylindole-1-carboxamideIC504.5 nMUS-8933099: Monocyclic pyridine derivative
6-(2-methoxyethoxy)-N-methyl-5-[[2-[[4-(1-methylpiperidin-4-yl)benzoyl]amino]-4-pyridinyl]oxy]indole-1-carboxamideIC505.1 nMUS-8933099: Monocyclic pyridine derivative
5-[[2-[[4-(1-ethylpiperidin-4-yl)benzoyl]amino]-4-pyridinyl]oxy]-6-methoxy-N-methylindole-1-carboxamideIC506.4 nMUS-8933099: Monocyclic pyridine derivative
Linked sulfated tetracyclitol, 3KD7.2 nM
Linked sulfated tetracyclitol, 7KD8 nM
Linked sulfated tetracyclitol, 2KD20.7 nM
Linked sulfated tetracyclitol, 4KD25.4 nM
Linked sulfated tetracyclitol, 5KD29.8 nM
Linked sulfated tetracyclitol, 6KD39 nM
Linked sulfated tetracyclitol, 8KD40.4 nM
Linked sulfated tetracyclitol, 10KD115 nM
Linked sulfated tetracyclitol, 9KD119 nM
Linked sulfated tetracyclitol, 11KD187 nM
1-(4-(3-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3h)IC50208 nM
TivozanibKD259 nM
1-(4-(4-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3i)IC50276 nM
1-(4-(3-(Trifluoromethyl)phenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3j)IC50307 nM
1-(4-(3,4-Dichlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3l)IC50344 nM
1-(4-(2-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3g)IC50357 nM
1-(4-(4-Nitrophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3f)IC50382 nM
1-(4-(2,4-Dimethylphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3m)IC50395 nM
1-(4-Phenylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3a)IC50400 nM
1-(4-(4-Fluorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3e)IC50403 nM
1-(4-(2-Fluorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3d)IC50409 nM
1-(4-(2,3-Dichlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3k)IC50409 nM
1-(4-(3-Chlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3c)IC50413 nM
1-(4-(2-Chlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3b)IC50418 nM
1-(4-Benzylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3n)IC50435 nM
1-(2-Methyl-1H-imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3u)IC50444 nM
1-(4-Methyl-1H-imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3v)IC50452 nM
1-(Dimethylamino)-3-(quinazolin-4-yloxy)propan-2-ol (3q)IC50455 nM
1-(4-Ethylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3p)IC50462 nM
1-(Piperidin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3s)IC50474 nM
1-(4-Methylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3o)IC50474 nM
1-Morpholino-3-(quinazolin-4-yloxy)propan-2-ol (3r)IC50483 nM
1-(1H-Imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3t)IC50483 nM

ChEMBL bioactivities

71 potent at pChembl≥5 of 83 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
8.35IC504.5nME-7090
8.33Kd4.7nMCHEMBL3559508
8.31Kd4.9nMCHEMBL3397498
8.29IC505.1nMCHEMBL3686883
8.28Kd5.2nMCHEMBL3409457
8.25Kd5.6nMCHEMBL3409454
8.19IC506.4nMCHEMBL3686864
8.09Kd8.2nMCHEMBL3409455
7.80Kd16nMCHEMBL3397488
7.80Kd16nMCHEMBL3409453
7.68Kd21nMCHEMBL3397494
7.64Kd23nMCHEMBL3397491
7.60Kd25nMCHEMBL3397487
7.46Kd35nMCHEMBL590011
7.44Kd36nMCHEMBL3397485
7.41Kd39nMCHEMBL2059243
7.39Kd41nMCHEMBL3397490
7.39Kd41nMCHEMBL3397489
7.37Kd43nMCHEMBL604368
7.32Kd48nMCHEMBL3559507
7.30Kd50nMCHEMBL2059502
7.28Kd52nMCHEMBL3397496
7.22Kd60nMCHEMBL3397495
7.21Kd62nMCHEMBL3397486
7.21Kd61nMMUPARFOSTAT SODIUM
7.17Kd68nMCHEMBL198643
7.14Kd73nMCHEMBL604570
7.09Kd82nMCHEMBL604366
7.08Kd84nMCHEMBL262707
7.08Kd83nMCHEMBL604568
7.07Kd86nMCHEMBL382044
7.07Kd86nMCHEMBL2029015
7.02Kd95nMCHEMBL3397493
7.02Kd95nMCHEMBL603122
7.00Kd99nMCHEMBL3397497
6.97Kd108nMCHEMBL2059242
6.96Kd110nMCHEMBL602307
6.95Kd112nMCHEMBL265885
6.89Kd129nMCHEMBL589773
6.89Kd130nMCHEMBL590012
6.85Kd140nMCHEMBL602114
6.83Kd147nMCHEMBL3397492
6.80Kd160nMCHEMBL2059241
6.80Kd160nMCHEMBL602113
6.80Kd160nMCHEMBL590010
6.60Kd253nMCHEMBL590013
6.51Kd311nMCHEMBL2059504
6.47IC50340nMCHEMBL2303729
6.41Kd390nMCHEMBL2059499
6.41Kd390nMCHEMBL2059500

PubChem BioAssay actives

100 with measured affinity, of 215 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.

CompoundAssayTypeValueUnit
(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2S,3S,4S,5R,6R)-6-[(2R,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfooxymethyl)oxan-4-yl]oxy-2-carboxy-4-hydroxy-5-sulfooxyoxan-3-yl]oxy-5-sulfooxy-6-(sulfooxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0047uM
pentasodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3-hydroxy-4,5-disulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0049uM
tetrasodium;[(2R,3R,4R,5R,6R)-5-acetamido-4-[(2R,3R,4R,5S,6S)-5-[(2S,3R,4R,5R,6R)-3-acetamido-4-[(2R,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxyoxan-2-yl]oxy-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-carboxy-3,4-dihydroxyoxan-2-yl]oxy-6-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-2-(sulfonatooxymethyl)oxan-3-yl] sulfate1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0052uM
trisodium;[(2R,3R,4R,5R,6R)-5-acetamido-4-[(2R,3R,4R,5S,6S)-5-[(2S,3R,4R,5R,6R)-3-acetamido-4-[(2R,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxyoxan-2-yl]oxy-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-carboxy-3,4-dihydroxyoxan-2-yl]oxy-6-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-2-(hydroxymethyl)oxan-3-yl] sulfate1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0056uM
trisodium;[(2R,3R,4R,5R,6R)-5-acetamido-4-[(2R,3R,4R,5S,6S)-5-[(2S,3R,4R,5R,6R)-3-acetamido-4-[(2R,3R,4S,5S,6S)-6-carboxy-3,4,5-trihydroxyoxan-2-yl]oxy-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-carboxy-3,4-dihydroxyoxan-2-yl]oxy-6-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-3-hydroxyoxan-2-yl]methyl sulfate1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0082uM
trisodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0160uM
pentasodium;[(2R,3R,4R,5R,6R)-5-acetamido-4-[(2R,3R,4S,5S,6S)-5-[(2S,3R,4R,5R,6R)-3-acetamido-4-[(2R,3R,4S,5S,6S)-6-carboxy-4,5-dihydroxy-3-sulfonatooxyoxan-2-yl]oxy-5-hydroxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-carboxy-4-hydroxy-3-sulfonatooxyoxan-2-yl]oxy-6-[6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-2-(sulfonatooxymethyl)oxan-3-yl] sulfate1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0160uM
tetrasodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-5-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0210uM
trisodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-5-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0230uM
disodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-4-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0250uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0350uM
disodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0360uM
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-[4-[[(3S,5S,8R,9S,10S,13R,14S,17R)-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxymethyl]triazol-1-yl]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] sulfate672590: Binding affinity to FGF-2 by surface plasmon resonance assaykd0.0390uM
trisodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-6-(hydroxymethyl)-5-sulfonatooxyoxan-4-yl]oxy-3,4-dihydroxy-5-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0410uM
trisodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-6-(hydroxymethyl)-5-sulfonatooxyoxan-4-yl]oxy-3,5-dihydroxy-4-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0410uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0430uM
(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2S,3S,4S,5R,6R)-6-[(2R,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfooxymethyl)oxan-4-yl]oxy-2-carboxy-4-hydroxy-5-sulfooxyoxan-3-yl]oxy-5-hydroxy-6-(sulfooxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-5-sulfooxyoxane-2-carboxylic acid1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor methodkd0.0480uM
tetradecasodium;[(2R,3R,4S,5R,6R)-2-[(2R,3R,4S,5R,6R)-6-[(2R,3R,4S,5R,6R)-6-[(2R,3R,4S,5R,6R)-6-[[(4R)-4-[(3S,5S,8R,9S,10S,12S,13R,14S,17R)-12-acetyloxy-10,13-dimethyl-3-sulfonatooxy-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-4,5-disulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-4,5-disulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-4,5-disulfonatooxy-2-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate672590: Binding affinity to FGF-2 by surface plasmon resonance assaykd0.0500uM
tetrasodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-6-(hydroxymethyl)-5-sulfonatooxyoxan-4-yl]oxy-3-hydroxy-4,5-disulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0520uM
tetrasodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-sulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-4-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0600uM
disodium;(2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-5-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0620uM
(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-triol256833: Binding affinity for FGF2 by BIAcore solution affinity assaykd0.0680uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0730uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0820uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0830uM
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]hexanamide256833: Binding affinity for FGF2 by BIAcore solution affinity assaykd0.0840uM
[(1R,2R,6R)-5-[bis[[bis[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]methyl]amino]-2,6-disulfonatooxycyclohex-3-en-1-yl] sulfate1799619: Binding Assay from Article 10.1002/cbic.200500089: “An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.”kd0.0850uM
(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-triol256833: Binding affinity for FGF2 by BIAcore solution affinity assaykd0.0860uM
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] sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0860uM
[(1R,2S,5R,6R)-2-[7-[bis[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]heptyl-[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]-5,6-disulfonatooxycyclohex-3-en-1-yl] sulfate1799619: Binding Assay from Article 10.1002/cbic.200500089: “An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.”kd0.0900uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.0950uM
trisodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3-hydroxy-4,5-disulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0950uM
tetrasodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3-hydroxy-4,5-disulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.0990uM
1-[4-(3-methoxyphenyl)piperazin-1-yl]-3-quinazolin-4-yloxypropan-2-ol1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.”ic500.1035uM
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-(octadecanoylamino)propoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate672590: Binding affinity to FGF-2 by surface plasmon resonance assaykd0.1080uM
[(1R,2S,5R,6R)-2-[8-[bis[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]octyl-[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]-5,6-disulfonatooxycyclohex-3-en-1-yl] sulfate1799619: Binding Assay from Article 10.1002/cbic.200500089: “An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.”kd0.1080uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1100uM
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-phenoxyacetamide256833: Binding affinity for FGF2 by BIAcore solution affinity assaykd0.1120uM
Tivozanib1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.”ic500.1141uM
1-[4-(4-methoxyphenyl)piperazin-1-yl]-3-quinazolin-4-yloxypropan-2-ol1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.”ic500.1218uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1290uM
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] sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1300uM
[(1R,2S,5R,6R)-2-[6-[bis[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]hexyl-[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]-5,6-disulfonatooxycyclohex-3-en-1-yl] sulfate1799619: Binding Assay from Article 10.1002/cbic.200500089: “An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.”kd0.1350uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1400uM
1-quinazolin-4-yloxy-3-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]propan-2-ol1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.”ic500.1447uM
trisodium;(2S,3R,4S,5R,6R)-6-[(2S,3R,4R,5R,6R)-3-acetamido-2-[(2R,3R,4R,5S)-6-[3-[5-(dithiolan-3-yl)pentanoylamino]anilino]-2,3,4,5-tetrahydroxyhexoxy]-5-hydroxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-4-sulfonatooxyoxane-2-carboxylate1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance methodkd0.1470uM
[(1R,2S,5R,6R)-2-[5-[bis[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]pentyl-[(1S,4R,5R,6R)-4,5,6-trisulfonatooxycyclohex-2-en-1-yl]amino]-5,6-disulfonatooxycyclohex-3-en-1-yl] sulfate1799619: Binding Assay from Article 10.1002/cbic.200500089: “An experimental and molecular-modeling study of the binding of linked sulfated tetracyclitols to FGF-1 and FGF-2.”kd0.1480uM
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 sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1600uM
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] sulfate459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assaykd0.1600uM
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-[[(3S,5S,8R,9S,10S,13R,14S,17R)-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]-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] sulfate672590: Binding affinity to FGF-2 by surface plasmon resonance assaykd0.1600uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Thalidomidedecreases activity, increases response to substance, affects expression, affects secretion, decreases expression (+1 more)6
sodium arsenitedecreases expression, increases expression5
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamidedecreases reaction, increases secretion, affects cotreatment, increases expression, decreases expression5
Benzo(a)pyreneaffects binding, decreases response to substance, decreases reaction, increases phosphorylation, affects methylation (+1 more)4
Tetrachlorodibenzodioxindecreases reaction, increases expression, affects expression4
Valproic Acidaffects expression, decreases expression4
SB 203580increases expression, decreases activity, decreases reaction, increases phosphorylation3
SU 5402decreases reaction, increases activity, increases expression, increases phosphorylation3
pyrazolanthronedecreases reaction, increases secretion, increases expression3
LDN 193189affects cotreatment, increases expression, decreases expression3
Cisplatinaffects reaction, decreases expression, affects cotreatment, decreases response to substance, increases expression3
Drugs, Chinese Herbaldecreases reaction, increases phosphorylation, increases expression3
Estradioldecreases expression, increases expression, affects cotreatment, affects binding3
Cyclosporineaffects cotreatment, affects expression, increases expression3
Asbestos, Crocidoliteincreases secretion, increases reaction, affects reaction, affects expression, increases expression3
Particulate Matterincreases abundance, increases expression, decreases secretion3
methylmercuric chloridedecreases expression2
bisphenol Adecreases expression, decreases methylation2
epigallocatechin gallatedecreases expression, affects cotreatment2
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-onedecreases reaction, increases activity, increases expression, increases phosphorylation2
entinostatincreases expression, affects cotreatment2
monomethylarsonous acidincreases expression2
Resveratroldecreases expression2
Zoledronic Acidincreases reaction, decreases expression2
Arsenic Trioxidedecreases reaction, increases phosphorylation, decreases expression2
Fulvestrantincreases expression, affects cotreatment, increases methylation, decreases reaction2
Gemcitabineaffects cotreatment, increases expression2
Acetylcysteinedecreases reaction, increases secretion, decreases expression2
Air Pollutantsaffects cotreatment, decreases expression, increases abundance, increases expression2
Cadmiumincreases abundance, increases expression, decreases expression2

ChEMBL screening assays

35 unique, capped per target: 35 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1003199BindingBinding affinity to biotinylated FGF2 in CHO cells by flow cytometryGuanidinylated neomycin delivers large, bioactive cargo into cells through a heparan sulfate-dependent pathway. — J Biol Chem

Cellosaurus cell lines

8 cell lines: 6 cancer cell line, 2 spontaneously immortalized cell line

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

CellosaurusNameCategorySex
CVCL_A9DWL-bFGF-5Spontaneously immortalized cell lineMale
CVCL_A9DXL-bFGF-6Spontaneously immortalized cell lineMale
CVCL_B8G0Abcam HCT 116 FGF2 KOCancer cell lineMale
CVCL_B9I7Abcam A-549 FGF2 KOCancer cell lineMale
CVCL_D8L8Ubigene HCT 116 FGF2 KOCancer cell lineMale
CVCL_E6ZQHCC827-TKCancer cell lineFemale
CVCL_SN48HAP1 FGF2 (-) 1Cancer cell lineMale
CVCL_SN49HAP1 FGF2 (-) 2Cancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT02513940PHASE4COMPLETEDInfluence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes
NCT03834883PHASE4COMPLETEDReducing the Risk of Drug-Induced QT Interval Lengthening in Women
NCT04169100PHASE4UNKNOWNNovel Form of Acquired Long QT Syndrome
NCT04675788PHASE4COMPLETEDNovel Approaches for Minimizing Drug-Induced QT Interval Lengthening
NCT04586348PHASE4UNKNOWNPrenatal Iodine Supplementation and Early Childhood Neurodevelopment
NCT04873115PHASE4UNKNOWNDouble-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties,
NCT02559102PHASE3COMPLETEDDexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants
NCT02757079PHASE3COMPLETEDStudy of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders
NCT06915480PHASE3RECRUITINGReducing Missed Appointments
NCT07377032PHASE3RECRUITINGTAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders
NCT01648205PHASE2COMPLETEDLong-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients
NCT02412709PHASE2UNKNOWNLong QT Syndrome Screening in Newborns
NCT04581408PHASE2COMPLETEDMutation-specific Therapy for the Long QT Syndrome
NCT02909959PHASE2COMPLETEDSulforaphane for the Treatment of Young Men With Autism Spectrum Disorder
NCT06081348PHASE2RECRUITINGSertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders
NCT06352372PHASE2COMPLETEDSafety and Efficacy of tPBM for Epileptiform Activity in Autism
NCT00316459PHASE1COMPLETEDStudy Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects
NCT01849003PHASE1COMPLETEDStudy of the Effect of GS-6615 in Subjects With LQT-3
NCT02365532PHASE1COMPLETEDEffect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults
NCT02412098PHASE1COMPLETEDPharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function
NCT02441829PHASE1COMPLETEDPharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function
NCT05759962PHASE1COMPLETEDPhase 1 Study of LQT-1213 in Healthy Adults
NCT00503191PHASE1COMPLETEDNeuroModulation Technique Treatment of Autism
NCT04475848PHASE1COMPLETEDA Study to Investigate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect of RO6953958 in Healthy Participants
NCT06300398PHASE1COMPLETEDIAMA-6 Oral Dose Study in Healthy Adults
NCT05906732PHASE1/PHASE2TERMINATEDStudy of LQT-1213 on QTc-induced Prolongation in Healthy Adult Subjects (Part1) and on Congenital Long QT in Patients Diagnosed With Type 2 or 3 Long QT Syndrome (Part 2).
NCT00005176Not specifiedCOMPLETEDLong QT Syndrome-Population Genetics and Cardiac Studies
NCT00005250Not specifiedCOMPLETEDLinkage Study of Long QT Syndrome In An Amish Kindred
NCT00005367Not specifiedCOMPLETEDEpidemiology of Long QTand Asian Sudden Death in Sleep
NCT00221832Not specifiedUNKNOWNMolecular Genetic Screening and Identification of Congenital Arrhythmogenic Diseases
NCT00292032Not specifiedCOMPLETEDRegistry of Unexplained Cardiac Arrest
NCT00335036Not specifiedTERMINATEDPediatric Lead Extractability and Survival Evaluation (PLEASE)
NCT00399412Not specifiedCOMPLETEDECG Signal Collection From Long QT Syndrome, Wide QRS Complexes, Heart Failure, and Cardiac Resynchronization Patients
NCT00488254Not specifiedCOMPLETEDThe Long QT Syndrome in Pregnancy
NCT00588965Not specifiedCOMPLETEDEffect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects
NCT01705925Not specifiedCOMPLETEDMulticenter Evaluation of Children and Young Adults With Genotype Positive Long QT Syndrome
NCT01903564Not specifiedCOMPLETEDFetal and Neonatal Magnetophysiology
NCT02082431Not specifiedCOMPLETEDDetermine the Incidence of Long QT Amongst a Large Cohort of Subjects Diagnosed With Unilateral or Bilateral Sensorineural Hearing Loss.
NCT02413450Not specifiedENROLLING_BY_INVITATIONDerivation of Human Induced Pluripotent Stem (iPS) Cells to Heritable Cardiac Arrhythmias
NCT02425189Not specifiedCOMPLETEDThe Canadian National Long QT Syndrome Registry
  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): irritable bowel syndrome