FGF2
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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
| Field | Value |
|---|---|
| HGNC ID | HGNC:3676 |
| Approved symbol | FGF2 |
| Name | fibroblast growth factor 2 |
| Location | 4q28.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000138685 |
| Ensembl biotype | protein_coding |
| OMIM | 134920 |
| Entrez | 2247 |
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
| Exon | Start | End |
|---|---|---|
| ENSE00000970285 | 122876321 | 122876424 |
| ENSE00001081614 | 122892211 | 122898236 |
| ENSE00003705888 | 122826831 | 122827352 |
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 ID | TPM avg | Samples expressed |
|---|---|---|
| 49546 | 38.4242 | 1259 |
| 49547 | 0.4712 | 260 |
| 49545 | 0.4297 | 252 |
Top tissues by expression
286 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cartilage tissue | UBERON:0002418 | 93.75 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 93.21 | gold quality |
| calcaneal tendon | UBERON:0003701 | 89.14 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 86.26 | gold quality |
| stromal cell of endometrium | CL:0002255 | 85.92 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 85.77 | gold quality |
| adipose tissue | UBERON:0001013 | 84.82 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 84.66 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 84.07 | gold quality |
| connective tissue | UBERON:0002384 | 84.03 | gold quality |
| thoracic aorta | UBERON:0001515 | 83.75 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 83.74 | gold quality |
| ascending aorta | UBERON:0001496 | 83.65 | gold quality |
| aorta | UBERON:0000947 | 82.88 | gold quality |
| right coronary artery | UBERON:0001625 | 82.79 | gold quality |
| islet of Langerhans | UBERON:0000006 | 82.41 | gold quality |
| body of uterus | UBERON:0009853 | 82.39 | gold quality |
| popliteal artery | UBERON:0002250 | 82.36 | gold quality |
| tibial artery | UBERON:0007610 | 82.35 | gold quality |
| mucosa of stomach | UBERON:0001199 | 82.29 | gold quality |
| caudate nucleus | UBERON:0001873 | 82.23 | gold quality |
| ventricular zone | UBERON:0003053 | 82.08 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 81.77 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 81.72 | gold quality |
| lower esophagus | UBERON:0013473 | 81.68 | gold quality |
| tibial nerve | UBERON:0001323 | 81.46 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 81.45 | gold quality |
| left coronary artery | UBERON:0001626 | 81.31 | gold quality |
| amygdala | UBERON:0001876 | 81.31 | gold quality |
| omental fat pad | UBERON:0010414 | 80.98 | gold quality |
Single-cell (SCXA)
Detected in 6 experiment(s), a significant marker in 4.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-7249 | yes | 18882.71 |
| E-MTAB-8559 | yes | 945.99 |
| E-MTAB-7052 | yes | 571.63 |
| E-ANND-3 | yes | 4.49 |
| E-CURD-10 | no | 263.65 |
| E-MTAB-6142 | no | 19.17 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
10 targets.
| Target | Regulation |
|---|---|
| ALPL | Repression |
| ANKH | Activation |
| BMP2 | Activation |
| ENPP1 | Activation |
| FGFR1 | Repression |
| GPC1 | Repression |
| HBA1 | Repression |
| HBB | Repression |
| MMP13 | Activation |
| TGFB1 | Activation |
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):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| HSA-MIR-450A-1-3P | 100.00 | 69.33 | 1837 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-3120-5P | 100.00 | 65.56 | 965 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-432-3P | 100.00 | 67.86 | 705 |
| HSA-MIR-4510 | 100.00 | 66.60 | 2050 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-3185 | 99.99 | 68.12 | 1959 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-223-3P | 99.99 | 70.14 | 1140 |
| HSA-MIR-511-3P | 99.99 | 68.85 | 1467 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-103A-3P | 99.98 | 69.14 | 1595 |
| HSA-MIR-107 | 99.98 | 69.14 | 1595 |
| HSA-MIR-4650-5P | 99.98 | 64.69 | 999 |
| HSA-MIR-568 | 99.98 | 69.86 | 2084 |
| HSA-MIR-499A-5P | 99.98 | 70.79 | 1323 |
| HSA-MIR-4803 | 99.98 | 71.99 | 3117 |
| HSA-MIR-25-3P | 99.98 | 74.60 | 1817 |
| HSA-MIR-363-3P | 99.98 | 74.72 | 1821 |
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
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Fgf2 | ENSMUSG00000037225 |
| rattus_norvegicus | Fgf2 | ENSRNOG00000017392 |
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 2 — P09038 (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 ID | Names | Canonical? |
|---|---|---|
| P09038-4 | 1 | yes |
| P09038-1 | 2 | |
| P09038-2 | 3 | |
| P09038-3 | 4 |
RefSeq proteins (2): NP_001348594, NP_001997 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR002209 | Fibroblast_GF_fam | Family |
| IPR008996 | IL1/FGF | Homologous_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.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8OM6 | X-RAY DIFFRACTION | 1.31 |
| 8HU7 | X-RAY DIFFRACTION | 1.4 |
| 8HUE | X-RAY DIFFRACTION | 1.48 |
| 4OEE | X-RAY DIFFRACTION | 1.5 |
| 1BFG | X-RAY DIFFRACTION | 1.6 |
| 4FGF | X-RAY DIFFRACTION | 1.6 |
| 4OEG | X-RAY DIFFRACTION | 1.6 |
| 2FGF | X-RAY DIFFRACTION | 1.77 |
| 4OEF | X-RAY DIFFRACTION | 1.8 |
| 1BAS | X-RAY DIFFRACTION | 1.9 |
| 1BFB | X-RAY DIFFRACTION | 1.9 |
| 5X1O | X-RAY DIFFRACTION | 1.9 |
| 1BFF | X-RAY DIFFRACTION | 2 |
| 1BFC | X-RAY DIFFRACTION | 2.2 |
| 1EV2 | X-RAY DIFFRACTION | 2.2 |
| 1FGA | X-RAY DIFFRACTION | 2.2 |
| 1IIL | X-RAY DIFFRACTION | 2.3 |
| 2BFH | X-RAY DIFFRACTION | 2.5 |
| 6L4O | X-RAY DIFFRACTION | 2.6 |
| 1II4 | X-RAY DIFFRACTION | 2.7 |
| 1CVS | X-RAY DIFFRACTION | 2.8 |
| 1FQ9 | X-RAY DIFFRACTION | 3 |
| 1BLA | SOLUTION NMR | |
| 1BLD | SOLUTION NMR | |
| 2M49 | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P09038-F1 | 72.18 | 0.47 |
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):
| Position | Phenotype |
|---|---|
| 181 | no effect on integrin binding. |
| 186 | no effect on integrin binding. |
| 188 | no effect on integrin binding. |
| 261–262 | abolishes binding to integrin itgav:itgb3 and suppresses fgf2 signaling with loss of erk1/2 activation and reduced abili |
| 267 | reduces 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
| ID | Pathway |
|---|---|
| R-HSA-109704 | PI3K Cascade |
| R-HSA-1257604 | PIP3 activates AKT signaling |
| R-HSA-1839122 | Signaling by activated point mutants of FGFR1 |
| R-HSA-1839130 | Signaling by activated point mutants of FGFR3 |
| R-HSA-190322 | FGFR4 ligand binding and activation |
| R-HSA-190370 | FGFR1b ligand binding and activation |
| R-HSA-190372 | FGFR3c ligand binding and activation |
| R-HSA-190373 | FGFR1c ligand binding and activation |
| R-HSA-190375 | FGFR2c ligand binding and activation |
| R-HSA-190377 | FGFR2b ligand binding and activation |
| R-HSA-2033519 | Activated point mutants of FGFR2 |
| R-HSA-2219530 | Constitutive Signaling by Aberrant PI3K in Cancer |
| R-HSA-2892247 | POU5F1 (OCT4), SOX2, NANOG activate genes related to proliferation |
| R-HSA-3000170 | Syndecan interactions |
| R-HSA-3000171 | Non-integrin membrane-ECM interactions |
| R-HSA-5654219 | Phospholipase C-mediated cascade: FGFR1 |
| R-HSA-5654221 | Phospholipase C-mediated cascade; FGFR2 |
| R-HSA-5654227 | Phospholipase C-mediated cascade; FGFR3 |
| R-HSA-5654228 | Phospholipase C-mediated cascade; FGFR4 |
| R-HSA-5654687 | Downstream signaling of activated FGFR1 |
| R-HSA-5654688 | SHC-mediated cascade:FGFR1 |
| R-HSA-5654689 | PI-3K cascade:FGFR1 |
| R-HSA-5654693 | FRS-mediated FGFR1 signaling |
| R-HSA-5654695 | PI-3K cascade:FGFR2 |
| R-HSA-5654699 | SHC-mediated cascade:FGFR2 |
| R-HSA-5654700 | FRS-mediated FGFR2 signaling |
| R-HSA-5654704 | SHC-mediated cascade:FGFR3 |
| R-HSA-5654706 | FRS-mediated FGFR3 signaling |
| R-HSA-5654710 | PI-3K cascade:FGFR3 |
| R-HSA-5654712 | FRS-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:
| Category | Pathways |
|---|---|
| FGFR1 ligand binding and activation | 2 |
| FGFR2 ligand binding and activation | 2 |
| IRS-mediated signalling | 1 |
| Intracellular signaling by second messengers | 1 |
| FGFR1 mutant receptor activation | 1 |
| FGFR3 mutant receptor activation | 1 |
| Signaling by FGFR4 | 1 |
| FGFR3 ligand binding and activation | 1 |
| FGFR2 mutant receptor activation | 1 |
| PI3K/AKT Signaling in Cancer | 1 |
| Transcriptional regulation of pluripotent stem cells | 1 |
| Non-integrin membrane-ECM interactions | 1 |
| Extracellular matrix organization | 1 |
| Downstream signaling of activated FGFR1 | 1 |
| Downstream signaling of activated FGFR2 | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| receptor ligand activity | 3 |
| cell differentiation | 2 |
| signaling receptor binding | 2 |
| cellular anatomical structure | 2 |
| ossification | 1 |
| branching morphogenesis of an epithelial tube | 1 |
| ureteric bud morphogenesis | 1 |
| regulation of animal organ formation | 1 |
| specification of animal organ identity | 1 |
| developmental induction | 1 |
| positive regulation of animal organ morphogenesis | 1 |
| epithelial cell proliferation | 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 |
| neuroblast proliferation | 1 |
| positive regulation of neurogenesis | 1 |
| regulation of neuroblast proliferation | 1 |
| positive regulation of neural precursor cell proliferation | 1 |
| DNA-templated transcription | 1 |
| response to chemical | 1 |
| taxis | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| small GTPase-mediated signal transduction | 1 |
| system development | 1 |
| generation of neurons | 1 |
| neural precursor cell proliferation | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| positive regulation of cellular process | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| cellular response to fibroblast growth factor stimulus | 1 |
| embryo development | 1 |
| anatomical structure morphogenesis | 1 |
Protein interactions and networks
STRING
5516 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| FGF2 | FGFR1 | P11362 | 998 |
| FGF2 | FGFR2 | P18443 | 997 |
| FGF2 | FGFR3 | P22607 | 997 |
| FGF2 | KDR | P35968 | 995 |
| FGF2 | HSPG2 | P98160 | 995 |
| FGF2 | FGFR4 | P22455 | 993 |
| FGF2 | CD44 | P16070 | 991 |
| FGF2 | SDC1 | P18827 | 988 |
| FGF2 | FLT1 | P16057 | 979 |
| FGF2 | FGFBP1 | Q14512 | 977 |
| FGF2 | TGFB1 | P01137 | 971 |
| FGF2 | SDC4 | P31431 | 971 |
| FGF2 | CX3CL1 | P78423 | 970 |
| FGF2 | EGF | P01133 | 969 |
| FGF2 | CCL11 | P50877 | 968 |
IntAct
80 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| FGF2 | FGFR1 | psi-mi:“MI:0407”(direct interaction) | 0.910 |
| FGFR1 | FGF2 | psi-mi:“MI:0407”(direct interaction) | 0.910 |
| FGF2 | PTX3 | psi-mi:“MI:0407”(direct interaction) | 0.790 |
| PTX3 | FGF2 | psi-mi:“MI:0407”(direct interaction) | 0.790 |
| FGF2 | PTX3 | psi-mi:“MI:0915”(physical association) | 0.790 |
| FGFR2 | FGF2 | psi-mi:“MI:0407”(direct interaction) | 0.780 |
| FGF2 | FGFR2 | psi-mi:“MI:0407”(direct interaction) | 0.780 |
| SDC2 | PDPK1 | psi-mi:“MI:0914”(association) | 0.640 |
| CAMKV | AP3B1 | psi-mi:“MI:0914”(association) | 0.640 |
| FGFBP1 | FGF2 | psi-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.
| A | Effect | B | Mechanism |
|---|---|---|---|
| FGF2 | up-regulates | MAPK14 | |
| FGF2 | up-regulates | RUNX2 | |
| FGF2 | “up-regulates quantity by expression” | BMP2 | “transcriptional regulation” |
| FGF2 | up-regulates | FGFR3 | binding |
| FGF2 | “up-regulates quantity by expression” | TGFB1 | “transcriptional regulation” |
| FGF2 | up-regulates | MAPK1 | |
| FGF2 | up-regulates | MAPK3 | |
| FGF2 | up-regulates | MAPK8 | |
| FGF2 | up-regulates | FGFR4 | binding |
| 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” |
| FGF2 | up-regulates | Gbeta | |
| FGF2 | up-regulates | ERK1/2 | |
| FGF2 | up-regulates | FGFR2 | binding |
| FGF2 | up-regulates | Angiogenesis |
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:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Defective B4GALT7 causes EDS, progeroid type | 7 | 117.6× | 9e-12 |
| Defective B3GAT3 causes JDSSDHD | 7 | 117.6× | 9e-12 |
| Defective B3GALT6 causes EDSP2 and SEMDJL1 | 7 | 117.6× | 9e-12 |
| Attachment and Entry | 6 | 106.1× | 6e-10 |
| HS-GAG degradation | 6 | 87.6× | 2e-09 |
| Respiratory syncytial virus (RSV) attachment and entry | 6 | 87.6× | 2e-09 |
| Initiation of coagulation cascade | 6 | 84.0× | 2e-09 |
| Glycosaminoglycan-protein linkage region biosynthesis | 7 | 81.1× | 9e-11 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| fibroblast growth factor receptor signaling pathway | 5 | 35.7× | 4e-05 |
| cell migration | 9 | 13.8× | 6e-06 |
| positive regulation of ERK1 and ERK2 cascade | 5 | 10.6× | 6e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
68 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 49 |
| Likely benign | 7 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 635942 | Single allele | Likely pathogenic |
SpliceAI
0 predictions. Top by Δscore:
AlphaMissense
999 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 4:122827269:T:A | L165Q | 1.000 |
| 4:122827269:T:C | L165P | 1.000 |
| 4:122827274:T:C | C167R | 1.000 |
| 4:122827275:G:A | C167Y | 1.000 |
| 4:122827276:C:G | C167W | 1.000 |
| 4:122827284:G:A | G170E | 1.000 |
| 4:122827292:T:C | F173L | 1.000 |
| 4:122827294:C:A | F173L | 1.000 |
| 4:122827294:C:G | F173L | 1.000 |
| 4:122827325:G:T | G184W | 1.000 |
| 4:122827326:G:A | G184E | 1.000 |
| 4:122876327:T:C | L195P | 1.000 |
| 4:122876363:T:A | I207N | 1.000 |
| 4:122876363:T:C | I207T | 1.000 |
| 4:122876363:T:G | I207S | 1.000 |
| 4:122876368:G:A | G209R | 1.000 |
| 4:122876368:G:C | G209R | 1.000 |
| 4:122876390:T:C | L216P | 1.000 |
| 4:122876408:G:A | G222E | 1.000 |
| 4:122876408:G:T | G222V | 1.000 |
| 4:122892236:T:C | F236S | 1.000 |
| 4:122892243:A:C | E238D | 1.000 |
| 4:122892243:A:T | E238D | 1.000 |
| 4:122892267:T:A | N246K | 1.000 |
| 4:122892267:T:G | N246K | 1.000 |
| 4:122892271:T:C | Y248H | 1.000 |
| 4:122892271:T:G | Y248D | 1.000 |
| 4:122892305:C:A | A259E | 1.000 |
| 4:122892319:G:T | G264W | 1.000 |
| 4:122892320:G:A | G264E | 1.000 |
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):
| Study | Trait | p-value |
|---|---|---|
| GCST002436_2 | Irritable bowel syndrome | 8.000000e-08 |
| GCST002782_12 | Waist-to-hip ratio adjusted for body mass index | 3.000000e-07 |
| GCST002782_13 | Waist-to-hip ratio adjusted for body mass index | 4.000000e-08 |
| GCST002782_14 | Waist-to-hip ratio adjusted for body mass index | 5.000000e-06 |
| GCST002782_15 | Waist-to-hip ratio adjusted for body mass index | 3.000000e-07 |
| GCST002783_80 | Body mass index | 7.000000e-07 |
| GCST004505_109 | Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour) | 8.000000e-06 |
| GCST004863_136 | Mosquito bite size | 4.000000e-08 |
| GCST007234_10 | Acne (severe) | 2.000000e-09 |
| GCST90020024_683 | A body shape index | 5.000000e-09 |
| GCST90020025_614 | Waist-to-hip ratio adjusted for BMI | 5.000000e-08 |
EFO canonical traits (5, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007788 | BMI-adjusted waist-hip ratio |
| EFO:0004340 | body mass index |
| EFO:0004318 | smoking behavior |
| EFO:0008378 | mosquito bite reaction size measurement |
| EFO:0007789 | BMI-adjusted waist circumference |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008133 | Long QT Syndrome | C14.280.067.565; C14.280.123.625; C16.131.240.400.715; C23.550.073.547 |
| D065886 | Neurodevelopmental Disorders | F03.625 |
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).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL3686884 | E-7090 | 2 | 77 |
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.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| Linked sulfated tetracyclitol, 12 | KD | 0.4 nM | |
| 5-[[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]-4-pyridinyl]oxy]-6-(2-methoxyethoxy)-N-methylindole-1-carboxamide | IC50 | 4.5 nM | US-8933099: Monocyclic pyridine derivative |
| 6-(2-methoxyethoxy)-N-methyl-5-[[2-[[4-(1-methylpiperidin-4-yl)benzoyl]amino]-4-pyridinyl]oxy]indole-1-carboxamide | IC50 | 5.1 nM | US-8933099: Monocyclic pyridine derivative |
| 5-[[2-[[4-(1-ethylpiperidin-4-yl)benzoyl]amino]-4-pyridinyl]oxy]-6-methoxy-N-methylindole-1-carboxamide | IC50 | 6.4 nM | US-8933099: Monocyclic pyridine derivative |
| Linked sulfated tetracyclitol, 3 | KD | 7.2 nM | |
| Linked sulfated tetracyclitol, 7 | KD | 8 nM | |
| Linked sulfated tetracyclitol, 2 | KD | 20.7 nM | |
| Linked sulfated tetracyclitol, 4 | KD | 25.4 nM | |
| Linked sulfated tetracyclitol, 5 | KD | 29.8 nM | |
| Linked sulfated tetracyclitol, 6 | KD | 39 nM | |
| Linked sulfated tetracyclitol, 8 | KD | 40.4 nM | |
| Linked sulfated tetracyclitol, 10 | KD | 115 nM | |
| Linked sulfated tetracyclitol, 9 | KD | 119 nM | |
| Linked sulfated tetracyclitol, 11 | KD | 187 nM | |
| 1-(4-(3-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3h) | IC50 | 208 nM | |
| Tivozanib | KD | 259 nM | |
| 1-(4-(4-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3i) | IC50 | 276 nM | |
| 1-(4-(3-(Trifluoromethyl)phenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3j) | IC50 | 307 nM | |
| 1-(4-(3,4-Dichlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3l) | IC50 | 344 nM | |
| 1-(4-(2-Methoxyphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3g) | IC50 | 357 nM | |
| 1-(4-(4-Nitrophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3f) | IC50 | 382 nM | |
| 1-(4-(2,4-Dimethylphenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3m) | IC50 | 395 nM | |
| 1-(4-Phenylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3a) | IC50 | 400 nM | |
| 1-(4-(4-Fluorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3e) | IC50 | 403 nM | |
| 1-(4-(2-Fluorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3d) | IC50 | 409 nM | |
| 1-(4-(2,3-Dichlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3k) | IC50 | 409 nM | |
| 1-(4-(3-Chlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3c) | IC50 | 413 nM | |
| 1-(4-(2-Chlorophenyl)piperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3b) | IC50 | 418 nM | |
| 1-(4-Benzylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3n) | IC50 | 435 nM | |
| 1-(2-Methyl-1H-imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3u) | IC50 | 444 nM | |
| 1-(4-Methyl-1H-imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3v) | IC50 | 452 nM | |
| 1-(Dimethylamino)-3-(quinazolin-4-yloxy)propan-2-ol (3q) | IC50 | 455 nM | |
| 1-(4-Ethylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3p) | IC50 | 462 nM | |
| 1-(Piperidin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3s) | IC50 | 474 nM | |
| 1-(4-Methylpiperazin-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3o) | IC50 | 474 nM | |
| 1-Morpholino-3-(quinazolin-4-yloxy)propan-2-ol (3r) | IC50 | 483 nM | |
| 1-(1H-Imidazol-1-yl)-3-(quinazolin-4-yloxy)propan-2-ol (3t) | IC50 | 483 nM |
ChEMBL bioactivities
71 potent at pChembl≥5 of 83 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (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 acid | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0047 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0049 | uM |
| 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] sulfate | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0052 | uM |
| 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] sulfate | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0056 | uM |
| 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 sulfate | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0082 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0160 | uM |
| 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] sulfate | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0160 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0210 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0230 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0250 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-naphthalen-1-yltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0350 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0360 | uM |
| hexadecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[3-[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] sulfate | 672590: Binding affinity to FGF-2 by surface plasmon resonance assay | kd | 0.0390 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0410 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0410 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-phenyltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0430 | uM |
| (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 acid | 1198808: Binding affinity to FGF2 (unknown origin) assessed as change in luminance intensity at at 25 degC by SPR imaging sensor method | kd | 0.0480 | uM |
| 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] sulfate | 672590: Binding affinity to FGF-2 by surface plasmon resonance assay | kd | 0.0500 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0520 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0600 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0620 | uM |
| (2R,3S,4S,5S,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-octoxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol | 256833: Binding affinity for FGF2 by BIAcore solution affinity assay | kd | 0.0680 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[12-(4-naphthalen-1-yltriazol-1-yl)dodecoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0730 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-octoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0820 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[3-(4-phenyltriazol-1-yl)propoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0830 | uM |
| 6-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-N-[(2S,3S,4S,5S,6R)-3-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[(2R,3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]hexanamide | 256833: Binding affinity for FGF2 by BIAcore solution affinity assay | kd | 0.0840 | uM |
| [(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] sulfate | 1799619: 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.” | kd | 0.0850 | uM |
| (2R,3S,4S,5S,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4S,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-phenylmethoxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol | 256833: Binding affinity for FGF2 by BIAcore solution affinity assay | kd | 0.0860 | uM |
| hexadecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[3-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]propoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0860 | uM |
| [(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] sulfate | 1799619: 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.” | kd | 0.0900 | uM |
| hexadecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-phenylmethoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.0950 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0950 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.0990 | uM |
| 1-[4-(3-methoxyphenyl)piperazin-1-yl]-3-quinazolin-4-yloxypropan-2-ol | 1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.” | ic50 | 0.1035 | uM |
| tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[3-(octadecanoylamino)propoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 672590: Binding affinity to FGF-2 by surface plasmon resonance assay | kd | 0.1080 | uM |
| [(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] sulfate | 1799619: 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.” | kd | 0.1080 | uM |
| tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-naphthalen-1-yltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1100 | uM |
| N-[(2S,3S,4S,5S,6R)-3-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-dihydroxy-6-(hydroxymethyl)-4-[(2R,3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]-2-phenoxyacetamide | 256833: Binding affinity for FGF2 by BIAcore solution affinity assay | kd | 0.1120 | uM |
| Tivozanib | 1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.” | ic50 | 0.1141 | uM |
| 1-[4-(4-methoxyphenyl)piperazin-1-yl]-3-quinazolin-4-yloxypropan-2-ol | 1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.” | ic50 | 0.1218 | uM |
| tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-phenylmethoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1290 | uM |
| tridecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[8-[[5-(dimethylamino)naphthalen-1-yl]sulfonylamino]octoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1300 | uM |
| [(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] sulfate | 1799619: 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.” | kd | 0.1350 | uM |
| tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-[8-(4-phenyltriazol-1-yl)octoxy]-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1400 | uM |
| 1-quinazolin-4-yloxy-3-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]propan-2-ol | 1801412: VEGFR2 Kinase Assay from Article 10.1111/cbdd.12596: “Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.” | ic50 | 0.1447 | uM |
| 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-carboxylate | 1192380: Binding affinity to basic fibroblast growth factor (unknown origin) using sugar chip immobilized compound by surface plasmon resonance method | kd | 0.1470 | uM |
| [(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] sulfate | 1799619: 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.” | kd | 0.1480 | uM |
| tridecasodium;[(2R,3R,4R,5S,6S)-5-[(2R,3S,4S,5R,6R)-4-[(2R,3S,4S,5R,6R)-3,5-disulfonatooxy-6-(sulfonatooxymethyl)-4-[(2R,3S,4S,5R,6R)-3,4,5-trisulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-2-yl]oxy-6-octoxy-3,4-disulfonatooxyoxan-2-yl]methyl sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1600 | uM |
| tridecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[(4-butylphenyl)methoxy]-4,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-3-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl]oxy-3,5-disulfonatooxy-6-(sulfonatooxymethyl)oxan-4-yl] sulfate | 459628: Binding affinity to FGF2 by surface plasmon-based solution affinity assay | kd | 0.1600 | uM |
| tridecasodium;[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2R,3S,4S,5R,6R)-2-[(2S,3S,4R,5R,6R)-2-[[(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] sulfate | 672590: Binding affinity to FGF-2 by surface plasmon resonance assay | kd | 0.1600 | uM |
CTD chemical–gene interactions
190 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Thalidomide | decreases activity, increases response to substance, affects expression, affects secretion, decreases expression (+1 more) | 6 |
| sodium arsenite | decreases expression, increases expression | 5 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | decreases reaction, increases secretion, affects cotreatment, increases expression, decreases expression | 5 |
| Benzo(a)pyrene | affects binding, decreases response to substance, decreases reaction, increases phosphorylation, affects methylation (+1 more) | 4 |
| Tetrachlorodibenzodioxin | decreases reaction, increases expression, affects expression | 4 |
| Valproic Acid | affects expression, decreases expression | 4 |
| SB 203580 | increases expression, decreases activity, decreases reaction, increases phosphorylation | 3 |
| SU 5402 | decreases reaction, increases activity, increases expression, increases phosphorylation | 3 |
| pyrazolanthrone | decreases reaction, increases secretion, increases expression | 3 |
| LDN 193189 | affects cotreatment, increases expression, decreases expression | 3 |
| Cisplatin | affects reaction, decreases expression, affects cotreatment, decreases response to substance, increases expression | 3 |
| Drugs, Chinese Herbal | decreases reaction, increases phosphorylation, increases expression | 3 |
| Estradiol | decreases expression, increases expression, affects cotreatment, affects binding | 3 |
| Cyclosporine | affects cotreatment, affects expression, increases expression | 3 |
| Asbestos, Crocidolite | increases secretion, increases reaction, affects reaction, affects expression, increases expression | 3 |
| Particulate Matter | increases abundance, increases expression, decreases secretion | 3 |
| methylmercuric chloride | decreases expression | 2 |
| bisphenol A | decreases expression, decreases methylation | 2 |
| epigallocatechin gallate | decreases expression, affects cotreatment | 2 |
| 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | decreases reaction, increases activity, increases expression, increases phosphorylation | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| monomethylarsonous acid | increases expression | 2 |
| Resveratrol | decreases expression | 2 |
| Zoledronic Acid | increases reaction, decreases expression | 2 |
| Arsenic Trioxide | decreases reaction, increases phosphorylation, decreases expression | 2 |
| Fulvestrant | increases expression, affects cotreatment, increases methylation, decreases reaction | 2 |
| Gemcitabine | affects cotreatment, increases expression | 2 |
| Acetylcysteine | decreases reaction, increases secretion, decreases expression | 2 |
| Air Pollutants | affects cotreatment, decreases expression, increases abundance, increases expression | 2 |
| Cadmium | increases abundance, increases expression, decreases expression | 2 |
ChEMBL screening assays
35 unique, capped per target: 35 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1003199 | Binding | Binding affinity to biotinylated FGF2 in CHO cells by flow cytometry | Guanidinylated 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):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A9DW | L-bFGF-5 | Spontaneously immortalized cell line | Male |
| CVCL_A9DX | L-bFGF-6 | Spontaneously immortalized cell line | Male |
| CVCL_B8G0 | Abcam HCT 116 FGF2 KO | Cancer cell line | Male |
| CVCL_B9I7 | Abcam A-549 FGF2 KO | Cancer cell line | Male |
| CVCL_D8L8 | Ubigene HCT 116 FGF2 KO | Cancer cell line | Male |
| CVCL_E6ZQ | HCC827-TK | Cancer cell line | Female |
| CVCL_SN48 | HAP1 FGF2 (-) 1 | Cancer cell line | Male |
| CVCL_SN49 | HAP1 FGF2 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
268 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT02513940 | PHASE4 | COMPLETED | Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes |
| NCT03834883 | PHASE4 | COMPLETED | Reducing the Risk of Drug-Induced QT Interval Lengthening in Women |
| NCT04169100 | PHASE4 | UNKNOWN | Novel Form of Acquired Long QT Syndrome |
| NCT04675788 | PHASE4 | COMPLETED | Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening |
| NCT04586348 | PHASE4 | UNKNOWN | Prenatal Iodine Supplementation and Early Childhood Neurodevelopment |
| NCT04873115 | PHASE4 | UNKNOWN | Double-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, |
| NCT02559102 | PHASE3 | COMPLETED | Dexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants |
| NCT02757079 | PHASE3 | COMPLETED | Study of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders |
| NCT06915480 | PHASE3 | RECRUITING | Reducing Missed Appointments |
| NCT07377032 | PHASE3 | RECRUITING | TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders |
| NCT01648205 | PHASE2 | COMPLETED | Long-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients |
| NCT02412709 | PHASE2 | UNKNOWN | Long QT Syndrome Screening in Newborns |
| NCT04581408 | PHASE2 | COMPLETED | Mutation-specific Therapy for the Long QT Syndrome |
| NCT02909959 | PHASE2 | COMPLETED | Sulforaphane for the Treatment of Young Men With Autism Spectrum Disorder |
| NCT06081348 | PHASE2 | RECRUITING | Sertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders |
| NCT06352372 | PHASE2 | COMPLETED | Safety and Efficacy of tPBM for Epileptiform Activity in Autism |
| NCT00316459 | PHASE1 | COMPLETED | Study Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects |
| NCT01849003 | PHASE1 | COMPLETED | Study of the Effect of GS-6615 in Subjects With LQT-3 |
| NCT02365532 | PHASE1 | COMPLETED | Effect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults |
| NCT02412098 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function |
| NCT02441829 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function |
| NCT05759962 | PHASE1 | COMPLETED | Phase 1 Study of LQT-1213 in Healthy Adults |
| NCT00503191 | PHASE1 | COMPLETED | NeuroModulation Technique Treatment of Autism |
| NCT04475848 | PHASE1 | COMPLETED | A Study to Investigate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect of RO6953958 in Healthy Participants |
| NCT06300398 | PHASE1 | COMPLETED | IAMA-6 Oral Dose Study in Healthy Adults |
| NCT05906732 | PHASE1/PHASE2 | TERMINATED | Study 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). |
| NCT00005176 | Not specified | COMPLETED | Long QT Syndrome-Population Genetics and Cardiac Studies |
| NCT00005250 | Not specified | COMPLETED | Linkage Study of Long QT Syndrome In An Amish Kindred |
| NCT00005367 | Not specified | COMPLETED | Epidemiology of Long QTand Asian Sudden Death in Sleep |
| NCT00221832 | Not specified | UNKNOWN | Molecular Genetic Screening and Identification of Congenital Arrhythmogenic Diseases |
| NCT00292032 | Not specified | COMPLETED | Registry of Unexplained Cardiac Arrest |
| NCT00335036 | Not specified | TERMINATED | Pediatric Lead Extractability and Survival Evaluation (PLEASE) |
| NCT00399412 | Not specified | COMPLETED | ECG Signal Collection From Long QT Syndrome, Wide QRS Complexes, Heart Failure, and Cardiac Resynchronization Patients |
| NCT00488254 | Not specified | COMPLETED | The Long QT Syndrome in Pregnancy |
| NCT00588965 | Not specified | COMPLETED | Effect of Beta-blocker Therapy on QTc Response in Exercise and Recovery in Normal Subjects |
| NCT01705925 | Not specified | COMPLETED | Multicenter Evaluation of Children and Young Adults With Genotype Positive Long QT Syndrome |
| NCT01903564 | Not specified | COMPLETED | Fetal and Neonatal Magnetophysiology |
| NCT02082431 | Not specified | COMPLETED | Determine the Incidence of Long QT Amongst a Large Cohort of Subjects Diagnosed With Unilateral or Bilateral Sensorineural Hearing Loss. |
| NCT02413450 | Not specified | ENROLLING_BY_INVITATION | Derivation of Human Induced Pluripotent Stem (iPS) Cells to Heritable Cardiac Arrhythmias |
| NCT02425189 | Not specified | COMPLETED | The Canadian National Long QT Syndrome Registry |
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): irritable bowel syndrome