EPHA7
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Also known as Hek11
Summary
EPHA7 (EPH receptor A7, HGNC:3390) is a protein-coding gene on chromosome 6q16.1, encoding Ephrin type-A receptor 7 (Q15375). Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells.
This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into 2 groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. Increased expression of this gene is associated with multiple forms of carcinoma. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 2045 — RefSeq curated summary.
At a glance
- Gene–disease (curated): neurodevelopmental disorder (Moderate, GenCC)
- GWAS associations: 19
- Clinical variants (ClinVar): 118 total
- Druggable target: yes — 29 molecules with ChEMBL bioactivity
- Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 3 cancer types
- MANE Select transcript:
NM_004440
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:3390 |
| Approved symbol | EPHA7 |
| Name | EPH receptor A7 |
| Location | 6q16.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Hek11 |
| Ensembl gene | ENSG00000135333 |
| Ensembl biotype | protein_coding |
| OMIM | 602190 |
| Entrez | 2045 |
Gene structure
Transcript identifiers
Ensembl transcripts: 23 — 10 protein_coding, 6 retained_intron, 5 protein_coding_CDS_not_defined, 2 nonsense_mediated_decay
ENST00000369297, ENST00000369303, ENST00000679565, ENST00000679915, ENST00000680082, ENST00000680190, ENST00000680224, ENST00000680473, ENST00000680550, ENST00000680608, ENST00000680813, ENST00000680896, ENST00000680953, ENST00000681130, ENST00000681287, ENST00000681503, ENST00000681532, ENST00000681647, ENST00000681729, ENST00000681798, ENST00000868213, ENST00000868214, ENST00000922908
RefSeq mRNA: 10 — MANE Select: NM_004440
NM_001288629, NM_001288630, NM_001376465, NM_001376466, NM_001376467, NM_001376468, NM_001376469, NM_001376470, NM_001376471, NM_004440
CCDS: CCDS5031, CCDS75494, CCDS93971, CCDS93972, CCDS93973, CCDS93974
Canonical transcript exons
ENST00000369303 — 17 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000918734 | 93410501 | 93411170 |
| ENSE00000974737 | 93414703 | 93414767 |
| ENSE00000974738 | 93358256 | 93358411 |
| ENSE00000974739 | 93356717 | 93357052 |
| ENSE00000974741 | 93269477 | 93269660 |
| ENSE00000974743 | 93263860 | 93263915 |
| ENSE00000974744 | 93259354 | 93259479 |
| ENSE00000974745 | 93258099 | 93258284 |
| ENSE00000974746 | 93257462 | 93257523 |
| ENSE00000974749 | 93246792 | 93246985 |
| ENSE00000974750 | 93245298 | 93245453 |
| ENSE00001084117 | 93264594 | 93264702 |
| ENSE00001309196 | 93272298 | 93272422 |
| ENSE00001449448 | 93240020 | 93243540 |
| ENSE00001941413 | 93419245 | 93419559 |
| ENSE00002370295 | 93255828 | 93256037 |
| ENSE00002398313 | 93254647 | 93254796 |
Expression profiles
Bgee: expression breadth ubiquitous, 184 present calls, max score 92.28.
FANTOM5 (CAGE): breadth broad, TPM avg 23.2118 / max 3181.6713, expressed in 670 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 74759 | 22.6787 | 665 |
| 74760 | 0.3976 | 171 |
| 74761 | 0.1355 | 66 |
Top tissues by expression
267 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cortical plate | UBERON:0005343 | 92.28 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 91.31 | gold quality |
| lower esophagus | UBERON:0013473 | 91.13 | gold quality |
| endothelial cell | CL:0000115 | 90.13 | gold quality |
| Brodmann (1909) area 23 | UBERON:0013554 | 88.92 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 86.87 | gold quality |
| middle temporal gyrus | UBERON:0002771 | 86.29 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 86.25 | gold quality |
| ganglionic eminence | UBERON:0004023 | 86.06 | gold quality |
| ventricular zone | UBERON:0003053 | 85.67 | gold quality |
| caput epididymis | UBERON:0004358 | 81.69 | gold quality |
| primary visual cortex | UBERON:0002436 | 80.83 | gold quality |
| embryo | UBERON:0000922 | 80.36 | gold quality |
| mucosa of stomach | UBERON:0001199 | 80.08 | gold quality |
| colonic epithelium | UBERON:0000397 | 79.53 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 79.14 | gold quality |
| calcaneal tendon | UBERON:0003701 | 78.62 | gold quality |
| urinary bladder | UBERON:0001255 | 76.53 | gold quality |
| cerebellar cortex | UBERON:0002129 | 75.80 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 75.74 | gold quality |
| cerebellum | UBERON:0002037 | 75.32 | gold quality |
| entorhinal cortex | UBERON:0002728 | 75.31 | gold quality |
| buccal mucosa cell | CL:0002336 | 75.03 | gold quality |
| nucleus accumbens | UBERON:0001882 | 74.92 | gold quality |
| large intestine | UBERON:0000059 | 74.82 | gold quality |
| colon | UBERON:0001155 | 74.77 | gold quality |
| occipital lobe | UBERON:0002021 | 74.65 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 74.56 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 74.52 | gold quality |
| prostate gland | UBERON:0002367 | 74.08 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-9388 | yes | 13.04 |
| E-ANND-3 | yes | 6.60 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): DLX5, GATA3, GSC, HOXA13, HOXD13, MSX2, PBX1, TOP2B
miRNA regulators (miRDB)
291 targeting EPHA7, 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-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-3924 | 100.00 | 72.09 | 2394 |
| HSA-MIR-12118 | 100.00 | 65.88 | 1270 |
| HSA-MIR-1277-5P | 100.00 | 73.95 | 5056 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-9-5P | 100.00 | 72.28 | 2361 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-196A-5P | 100.00 | 68.16 | 684 |
| HSA-MIR-196B-5P | 100.00 | 68.16 | 681 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-4668-3P | 100.00 | 68.74 | 2635 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-4533 | 100.00 | 69.48 | 2758 |
| HSA-MIR-5692B | 100.00 | 71.32 | 2622 |
| HSA-MIR-5692C | 100.00 | 71.32 | 2622 |
| HSA-MIR-6740-5P | 100.00 | 65.64 | 932 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-3185 | 99.99 | 68.12 | 1959 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
| HSA-MIR-8068 | 99.98 | 73.85 | 2376 |
| HSA-MIR-3173-3P | 99.98 | 66.49 | 1217 |
| HSA-MIR-6891-5P | 99.98 | 66.53 | 1372 |
| HSA-MIR-103A-3P | 99.98 | 69.14 | 1595 |
Literature-anchored findings (GeneRIF, showing 35)
- downregulation of an Eph family gene in a solid tumor via aberrant 5’CpG island methylation, providing evidence that EphA7 gene is involved in human colorectal carcinogenesis (PMID:16007213)
- EphA7 expression in 52 gastric carcinoma was consistent with its transcript expression, with the protein being significantly overexpressed in younger patients (P = .016) and in patients with advanced tumors (P = .033) (PMID:17669470)
- siRNA-mediated suppression of ALL1/AF4 in SEMK2 cells carrying the t(4;11) chromosome translocation resulted in down-regulation of EphA7 (PMID:17726105)
- EphA7 protein may have a role in progression of glioblastoma multiforme (PMID:18366728)
- epigenetic inactivation of EphA7 may be involved in prostate carcinogenesis (PMID:18821581)
- Eph-A5 and Eph-A7 staining intensity was identified as independent prognostic factors for pancreatic ductal adenocarcinoma (PMID:19949912)
- analysis of the secreted form of EphA7 in lung cancer (PMID:20126984)
- EphA7 protein expression is significantly correlated with the biological behavior of primary hepatocellular carcinoma. (PMID:20302756)
- Data shew that the identification of three novel candidates as EPH receptor genes might indicate a link between perturbed compartmentalization of early neoplastic lesions and breast cancer risk and progression. (PMID:21124932)
- The expression of EphA7 and/or MTDH might be closely related to the carcinogenesis, progression, clinical biological behaviors and prognosis of gallbladder adenocarcinoma. (PMID:21609571)
- Data found significant correlations between ephA2, ephA4, ephA7, ephB4, and ephB6 and overall and/or recurrence-free survival in large microarray datasets. (PMID:21935409)
- MTDH and EphA7 are markers for metastasis and poor prognosis of gallbladder adenocarcinoma. (PMID:21964981)
- EPHA7 acts as a tumor suppressor in vivo and is targeted by genomic deletions and differential epigenetic silencing in human lymphomas. (PMID:22036564)
- Overexpression of EphA7 and/or MTDH might indicate poor prognosis in squamous cell cancer of the tongue. (PMID:22246354)
- miR-137 is able to directly bind to the EPHA7 3’UTR and negatively regulate the expression of EPHA7 in HUVECs. (PMID:24927112)
- Authors observed that the extracellular region of the EphA7 receptor was critical for interacting with caspase-8, whereas the cytoplasmic region of EphA7 was not. (PMID:25855521)
- Depletion of EphA7 remarkably inhibited the proliferation and invasion of Hep-2 and AMC-HN-8 cells in comparison to control and EphA7 siRNA negative control (NC)-transfected cells. (PMID:25968442)
- Eph receptor A7 may have an important role in the pathogenesis of nonsmall cell lung cancer by regulating PTEN expression via thephosphatase and tensin homolog/AKT pathway. (PMID:26936314)
- We have demonstrated the physical association and cellular co-localization of EPHA7 and EPHA10 in breast carcinoma cells. The nuclear co-localization of these two receptors in invasive MDA-MB-231 cells suggests their involvement in transcriptional activation of genes involved in invasiveness. (PMID:27566654)
- the interactions of EphA5/ephrinA5 and/or EphA7/ephrinA5 between HSPCs and BMSCs, independently and cooperatively, play a role in HSPC colony formation through the upregulation of GM-CSFR. Furthermore, the adhesion/migration of HSPCs appears to be mediated in part through the activation of Rac1. (PMID:27988259)
- receptor phosphorylation of EphA7, at least in part, suppress prostate cancer tumor malignancy through targeting PI3K/Akt signaling pathways. (PMID:29022918)
- EPHA7 is a positive upstream factor of C/EBPbeta contributing to the transcription and translation of KLF4, promoting ovulation via ADAMTS1. We demonstrated the functional role of EPHA7 in PCOS, which explains how the loss of EPHA7 underlies the ovulatory dysfunction. (PMID:30292674)
- Endogenously expressed EPH receptor A7 (EphA7) in BJAB B cells is critical for the cell-to-cell transmission of Kaposi’s sarcoma-associated herpesvirus (KSHV) from producer iSLK cells to BJAB target cells. Endogenous EphA7 is precipitated from the cellular lysate of BJAB cells using recombinant gH/gL, and knockout of EphA7 reduces transmission of KSHV into BJAB target cells. (PMID:31118261)
- SNHG14 serves as a facilitator in colorectal carcer through targeting EZH2-repressed EPHA7. (PMID:31273190)
- relationship between colorectal carcinoma and the four biomarkers CCL5, CCR5, PDGF, and EphA7 (PMID:31505877)
- Long noncoding RNA KCNQ1OT1 promotes proliferation, migration, and invasion in maxillary sinus squamous cell carcinoma by regulating miR-204/EphA7 axis. (PMID:31709597)
- Circulating microRNA-944 and its target gene EPHA7 as a potential biomarker for colorectal cancer. (PMID:32421395)
- MicroRNA-448/EPHA7 axis regulates cell proliferation, invasion and migration via regulation of PI3K/AKT signaling pathway and epithelial-to-mesenchymal transition in non-small cell lung cancer. (PMID:32572879)
- Identification of the soluble EphA7-interacting protein Nicalin as a regulator of EphA7 expression. (PMID:32914261)
- miR18a5p promotes melanoma cell proliferation and inhibits apoptosis and autophagy by targeting EPHA7 signaling. (PMID:33236144)
- Down-regulation of HCP5 inhibits cell proliferation, migration, and invasion through regulating EPHA7 by competitively binding miR-101 in osteosarcoma. (PMID:33439936)
- EPHA7 haploinsufficiency is associated with a neurodevelopmental disorder. (PMID:34176129)
- Crystal structure of clinically reported mutations Gly656Arg, Gly656Glu and Asp751His identified in the kinase domain of EphA7. (PMID:34186436)
- The identification and validation of EphA7 hypermethylation, a novel biomarker, in cervical cancer. (PMID:35681118)
- STAT3-EphA7 axis contributes to the progression of esophageal squamous cell carcinoma. (PMID:37738252)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Epha7 | ENSMUSG00000028289 |
| rattus_norvegicus | Epha7 | ENSRNOG00000007030 |
Paralogs (53): INSRR (ENSG00000027644), MUSK (ENSG00000030304), FLT4 (ENSG00000037280), EPHA3 (ENSG00000044524), ROS1 (ENSG00000047936), LTK (ENSG00000062524), ERBB3 (ENSG00000065361), TIE1 (ENSG00000066056), FGFR2 (ENSG00000066468), FGFR3 (ENSG00000068078), EPHA8 (ENSG00000070886), FGFR1 (ENSG00000077782), EPHA6 (ENSG00000080224), TYRO3 (ENSG00000092445), FLT1 (ENSG00000102755), MET (ENSG00000105976), EPHB6 (ENSG00000106123), PDGFRB (ENSG00000113721), EPHA4 (ENSG00000116106), TEK (ENSG00000120156), FLT3 (ENSG00000122025), KDR (ENSG00000128052), EPHB2 (ENSG00000133216), PDGFRA (ENSG00000134853), IGF1R (ENSG00000140443), NTRK3 (ENSG00000140538), ERBB2 (ENSG00000141736), EPHA2 (ENSG00000142627), EPHA5 (ENSG00000145242), EGFR (ENSG00000146648), EPHA1 (ENSG00000146904), NTRK2 (ENSG00000148053), MERTK (ENSG00000153208), EPHB1 (ENSG00000154928), KIT (ENSG00000157404), FGFR4 (ENSG00000160867), DDR2 (ENSG00000162733), RYK (ENSG00000163785), MST1R (ENSG00000164078), LMTK2 (ENSG00000164715)
Protein
Protein identifiers
Ephrin type-A receptor 7 — Q15375 (reviewed: Q15375)
Alternative names: EPH homology kinase 3, EPH-like kinase 11
All UniProt accessions (7): A0A7P0T9G1, A0A7P0T9L5, A0A7P0T9V9, A0A7P0TA58, A0A7P0TB85, A0A7P0TBL4, Q15375
UniProt curated annotations — full annotation on UniProt →
Function. Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Among GPI-anchored ephrin-A ligands, EFNA5 is a cognate/functional ligand for EPHA7 and their interaction regulates brain development modulating cell-cell adhesion and repulsion. Has a repellent activity on axons and is for instance involved in the guidance of corticothalamic axons and in the proper topographic mapping of retinal axons to the colliculus. May also regulate brain development through a caspase(CASP3)-dependent proapoptotic activity. Forward signaling may result in activation of components of the ERK signaling pathway including MAP2K1, MAP2K2, MAPK1 and MAPK3 which are phosphorylated upon activation of EPHA7.
Subunit / interactions. Heterotetramer upon binding of the ligand. The heterotetramer is composed of an ephrin dimer and a receptor dimer. Oligomerization is probably required to induce biological responses. Interacts (via PDZ-binding motif) with GRIP1 and PICK1 (via PDZ domain).
Subcellular location. Cell membrane.
Tissue specificity. Widely expressed.
Post-translational modifications. Phosphorylated.
Miscellaneous. May be due to a competing donor splice site. Expressed in lung cancer cells, lacks the kinase domain and is most probably secreted.
Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. Ephrin receptor subfamily.
Isoforms (5)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q15375-1 | 1, EPHA7-FL | yes |
| Q15375-2 | 2 | |
| Q15375-3 | 3 | |
| Q15375-4 | 4 | |
| Q15375-5 | 5, EPHA7-S |
RefSeq proteins (9): NP_001275558, NP_001275559, NP_001363394, NP_001363395, NP_001363396, NP_001363397, NP_001363399, NP_001363400, NP_004431* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR001090 | EPH_LBD | Domain |
| IPR001245 | Ser-Thr/Tyr_kinase_cat_dom | Domain |
| IPR001426 | Tyr_kinase_rcpt_V_CS | Conserved_site |
| IPR001660 | SAM | Domain |
| IPR003961 | FN3_dom | Domain |
| IPR008266 | Tyr_kinase_AS | Active_site |
| IPR008979 | Galactose-bd-like_sf | Homologous_superfamily |
| IPR009030 | Growth_fac_rcpt_cys_sf | Homologous_superfamily |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR011641 | Tyr-kin_ephrin_A/B_rcpt-like | Domain |
| IPR013761 | SAM/pointed_sf | Homologous_superfamily |
| IPR013783 | Ig-like_fold | Homologous_superfamily |
| IPR016257 | EPH | Family |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
| IPR020635 | Tyr_kinase_cat_dom | Domain |
| IPR027936 | EPH_TM | Domain |
| IPR034283 | EphA7_rcpt_lig-bd | Domain |
| IPR036116 | FN3_sf | Homologous_superfamily |
| IPR050449 | Ephrin_rcpt_TKs | Family |
Pfam: PF00041, PF00536, PF01404, PF07699, PF07714, PF14575, PF25599
Enzyme classification (BRENDA):
- EC 2.7.10.1 — receptor protein-tyrosine kinase (BRENDA: 44 organisms, 214 substrates, 574 inhibitors, 11 Km, 0 kcat entries)
Substrate kinetics (BRENDA)
4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.0011–0.129 | 4 |
| AC-DYFE-6-CHLORO-W-NHME | 0.0051 | 1 |
| AC-DYFGW-NHME | 0.07 | 1 |
| YFEW | 0.232 | 1 |
Catalyzed reactions (Rhea), 1 shown:
- L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
UniProt features (80 total): strand 22, helix 22, splice variant 6, sequence variant 6, domain 5, modified residue 4, turn 3, binding site 2, glycosylation site 2, topological domain 2, signal peptide 1, chain 1, short sequence motif 1, active site 1, transmembrane region 1, sequence conflict 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2REI | X-RAY DIFFRACTION | 1.6 |
| 3DKO | X-RAY DIFFRACTION | 2 |
| 3H8M | X-RAY DIFFRACTION | 2.1 |
| 3NRU | X-RAY DIFFRACTION | 2.3 |
| 7EEF | X-RAY DIFFRACTION | 2.6 |
| 7EED | X-RAY DIFFRACTION | 3.05 |
| 7EEC | X-RAY DIFFRACTION | 3.1 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q15375-F1 | 82.09 | 0.51 |
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 (1): 758 (proton acceptor)
Ligand- & substrate-binding residues (2): 639–647; 665
Post-translational modifications (4): 608, 614, 791, 940
Glycosylation sites (2): 343, 410
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-2682334 | EPH-Ephrin signaling |
| R-HSA-3928663 | EPHA-mediated growth cone collapse |
| R-HSA-3928665 | EPH-ephrin mediated repulsion of cells |
MSigDB gene sets: 437 (showing top):
GSE18804_SPLEEN_MACROPHAGE_VS_BRAIN_TUMORAL_MACROPHAGE_DN, GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, AAGCAAT_MIR137, GOBP_EPITHELIUM_DEVELOPMENT, YAATNRNNNYNATT_UNKNOWN, ACTACCT_MIR196A_MIR196B, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT, GOBP_REGULATION_OF_COLLATERAL_SPROUTING, GOBP_REGULATION_OF_PHOSPHORYLATION, MODULE_255, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, GOBP_SYNAPSE_ASSEMBLY, RORA1_01, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, GOBP_RETINAL_GANGLION_CELL_AXON_GUIDANCE
GO Biological Process (24): axon guidance (GO:0007411), brain development (GO:0007420), phosphorylation (GO:0016310), regulation of cell-cell adhesion (GO:0022407), retinal ganglion cell axon guidance (GO:0031290), regulation of protein autophosphorylation (GO:0031952), positive regulation of neuron apoptotic process (GO:0043525), ephrin receptor signaling pathway (GO:0048013), negative regulation of collateral sprouting (GO:0048671), branching morphogenesis of a nerve (GO:0048755), regulation of peptidyl-tyrosine phosphorylation (GO:0050730), modulation of chemical synaptic transmission (GO:0050804), negative chemotaxis (GO:0050919), neuron apoptotic process (GO:0051402), negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051898), negative regulation of synapse assembly (GO:0051964), regulation of ERK1 and ERK2 cascade (GO:0070372), nephric duct morphogenesis (GO:0072178), regulation of postsynapse organization (GO:0099175), protein phosphorylation (GO:0006468), apoptotic process (GO:0006915), cell surface receptor protein tyrosine kinase signaling pathway (GO:0007169), nervous system development (GO:0007399), positive regulation of apoptotic process (GO:0043065)
GO Molecular Function (15): protein tyrosine kinase activity (GO:0004713), GPI-linked ephrin receptor activity (GO:0005004), transmembrane-ephrin receptor activity (GO:0005005), ATP binding (GO:0005524), axon guidance receptor activity (GO:0008046), growth factor binding (GO:0019838), chemorepellent activity (GO:0045499), ephrin receptor binding (GO:0046875), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), transmembrane receptor protein tyrosine kinase activity (GO:0004714), ephrin receptor activity (GO:0005003), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (11): plasma membrane (GO:0005886), dendrite (GO:0030425), neuromuscular junction (GO:0031594), neuronal cell body (GO:0043025), Schaffer collateral - CA1 synapse (GO:0098685), hippocampal mossy fiber to CA3 synapse (GO:0098686), postsynaptic density membrane (GO:0098839), glutamatergic synapse (GO:0098978), membrane (GO:0016020), postsynaptic membrane (GO:0045211), postsynaptic specialization membrane (GO:0099634)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| EPH-Ephrin signaling | 2 |
| Axon guidance | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| synapse | 3 |
| axon guidance | 2 |
| regulation of protein phosphorylation | 2 |
| ephrin receptor activity | 2 |
| postsynaptic membrane | 2 |
| synaptic membrane | 2 |
| axonogenesis | 1 |
| neuron projection guidance | 1 |
| central nervous system development | 1 |
| animal organ development | 1 |
| head development | 1 |
| phosphate-containing compound metabolic process | 1 |
| regulation of cell adhesion | 1 |
| cell-cell adhesion | 1 |
| regulation of protein kinase activity | 1 |
| protein autophosphorylation | 1 |
| positive regulation of apoptotic process | 1 |
| regulation of neuron apoptotic process | 1 |
| neuron apoptotic process | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| negative regulation of cell growth | 1 |
| negative regulation of developmental growth | 1 |
| collateral sprouting | 1 |
| regulation of collateral sprouting | 1 |
| negative regulation of axonogenesis | 1 |
| morphogenesis of a branching structure | 1 |
| nervous system development | 1 |
| peptidyl-tyrosine phosphorylation | 1 |
| chemical synaptic transmission | 1 |
| regulation of trans-synaptic signaling | 1 |
| chemotaxis | 1 |
| apoptotic process | 1 |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 1 |
| regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 1 |
| negative regulation of intracellular signal transduction | 1 |
| synapse assembly | 1 |
| negative regulation of nervous system development | 1 |
| regulation of synapse assembly | 1 |
| negative regulation of cell junction assembly | 1 |
| negative regulation of synapse organization | 1 |
Protein interactions and networks
STRING
2302 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| EPHA7 | EFNA5 | P52803 | 995 |
| EPHA7 | EFNA2 | O43921 | 915 |
| EPHA7 | EFNA1 | P20827 | 914 |
| EPHA7 | EFNA3 | P52797 | 909 |
| EPHA7 | EFNA4 | P52798 | 787 |
| EPHA7 | EFNB2 | P52799 | 749 |
| EPHA7 | EPHA10 | Q5JZY3 | 659 |
| EPHA7 | EFNB1 | P98172 | 614 |
| EPHA7 | EFNB3 | Q15768 | 612 |
| EPHA7 | AFDN | P55196 | 591 |
| EPHA7 | CTNNB1 | P35222 | 509 |
| EPHA7 | NTRK2 | Q16620 | 496 |
| EPHA7 | NOTCH3 | Q9UM47 | 494 |
| EPHA7 | EPHA3 | P29320 | 490 |
| EPHA7 | CASP8 | Q14790 | 476 |
IntAct
201 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| EPHA7 | EPHA2 | psi-mi:“MI:0915”(physical association) | 0.780 |
| EPHA2 | EPHA7 | psi-mi:“MI:0915”(physical association) | 0.780 |
| EPHA2 | EPHA7 | psi-mi:“MI:0407”(direct interaction) | 0.780 |
| EPHA3 | EPHA7 | psi-mi:“MI:0407”(direct interaction) | 0.670 |
| EPHA7 | EFNA5 | psi-mi:“MI:0407”(direct interaction) | 0.590 |
| EPHA7 | GORASP2 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | LIN7C | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | DLG1 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| SCRIB | EPHA7 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| CASK | EPHA7 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | SCRIB | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | MPP7 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | GOPC | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| EPHA7 | PTPN13 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
| Efna1 | EPHA7 | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| EPHA7 | Efna1 | psi-mi:“MI:0407”(direct interaction) | 0.560 |
| EPHA7 | EPHB4 | psi-mi:“MI:0915”(physical association) | 0.540 |
| RYK | PCDH7 | psi-mi:“MI:0914”(association) | 0.530 |
| PICK1 | ILVBL | psi-mi:“MI:0914”(association) | 0.530 |
| TMEM30B | KLRG2 | psi-mi:“MI:0914”(association) | 0.530 |
| EPHA2 | GOLIM4 | psi-mi:“MI:0914”(association) | 0.530 |
| TMX1 | NRP1 | psi-mi:“MI:0914”(association) | 0.530 |
| CACNG2 | CCNT1 | psi-mi:“MI:0914”(association) | 0.530 |
| SLC9A8 | ZNF432 | psi-mi:“MI:0914”(association) | 0.530 |
| PICK1 | ATP6AP2 | psi-mi:“MI:0914”(association) | 0.530 |
| ANKH | FAM234B | psi-mi:“MI:0914”(association) | 0.530 |
| CSF1R | EPHB2 | psi-mi:“MI:0914”(association) | 0.500 |
| EPHA7 | EPHB2 | psi-mi:“MI:0915”(physical association) | 0.500 |
| EPHA7 | CSF1R | psi-mi:“MI:0915”(physical association) | 0.500 |
BioGRID (362): EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA7 (Proximity Label-MS), EPHA10 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), EPHA3 (Affinity Capture-MS), EFNA5 (Affinity Capture-MS), EPHA7 (Affinity Capture-MS), BCAM (Affinity Capture-MS), EPHA7 (Affinity Capture-MS)
ESM2 similar proteins: A0JM20, F1LW30, O73875, O73878, P00545, P07333, P11362, P13369, P16092, P18460, P21709, P21803, P21804, P22182, P22455, P22607, P29317, P54755, P54756, P54757, P54759, P54761, P55144, P55146, P57097, Q03142, Q04589, Q06418, Q06806, Q12866, Q15375, Q1KL86, Q498D6, Q60629, Q60750, Q60805, Q61772, Q61851, Q6UXZ4, Q8K1S2
Diamond homologs: G5EF96, O09127, O15197, O42422, P0C0K6, P16144, P29320, P29322, P43146, P54759, P70211, P97603, P97798, Q15375, Q24372, Q4ZHG4, Q61772, Q63155, Q8C310, Q90610, Q91736, Q91845, Q92859, A0JNB0, A1Y2K1, A2VDU3, A7J1T0, A7J1T2, A7MBB4, A8X775, D3ZG83, F4JTP5, H2KZW3, O01700, O08680, O13146, O13148, O22558, O43283, O43318
SIGNOR signaling
9 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| HOXA13 | “up-regulates quantity by expression” | EPHA7 | “transcriptional regulation” |
| HOXD13 | “up-regulates quantity by expression” | EPHA7 | “transcriptional regulation” |
| TOP2B | “up-regulates quantity by expression” | EPHA7 | “transcriptional regulation” |
| EPHA7 | “up-regulates activity” | EPHA10 | phosphorylation |
| EFNA2 | up-regulates | EPHA7 | binding |
| EFNA3 | up-regulates | EPHA7 | binding |
| EFNA1 | up-regulates | EPHA7 | binding |
| GSC | “down-regulates quantity by repression” | EPHA7 | “transcriptional regulation” |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 176 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 |
|---|---|---|---|
| Ras activation upon Ca2+ influx through NMDA receptor | 6 | 27.4× | 1e-05 |
| Unblocking of NMDA receptors, glutamate binding and activation | 6 | 26.1× | 1e-05 |
| Negative regulation of NMDA receptor-mediated neuronal transmission | 6 | 26.1× | 1e-05 |
| Long-term potentiation | 6 | 22.8× | 2e-05 |
| Assembly and cell surface presentation of NMDA receptors | 11 | 22.3× | 9e-10 |
| Dopamine Neurotransmitter Release Cycle | 5 | 19.9× | 3e-04 |
| Neurotransmitter release cycle | 5 | 17.6× | 5e-04 |
| Neurexins and neuroligins | 11 | 17.3× | 9e-09 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| establishment or maintenance of epithelial cell apical/basal polarity | 8 | 28.2× | 4e-07 |
| protein localization to synapse | 6 | 27.9× | 2e-05 |
| receptor clustering | 7 | 26.5× | 4e-06 |
| regulation of postsynaptic membrane neurotransmitter receptor levels | 5 | 15.0× | 2e-03 |
| ephrin receptor signaling pathway | 6 | 12.5× | 1e-03 |
| positive regulation of protein localization to plasma membrane | 6 | 9.9× | 3e-03 |
| cell-cell adhesion | 11 | 6.8× | 2e-04 |
| protein-containing complex assembly | 9 | 6.2× | 2e-03 |
Disease & clinical
Cancer significance
From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 3 cancer types — COADREAD, HCC, LUAD.
Clinical variants and AI predictions
ClinVar
118 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 97 |
| Likely benign | 4 |
| Benign | 5 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3555 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 6:93245296:A:AC | donor_gain | 1.0000 |
| 6:93245297:C:CG | donor_gain | 1.0000 |
| 6:93245297:CT:C | donor_gain | 1.0000 |
| 6:93245300:A:AC | donor_gain | 1.0000 |
| 6:93245301:A:C | donor_gain | 1.0000 |
| 6:93245308:T:TA | donor_gain | 1.0000 |
| 6:93245355:T:C | donor_gain | 1.0000 |
| 6:93254646:CAT:C | donor_gain | 1.0000 |
| 6:93254693:A:C | donor_gain | 1.0000 |
| 6:93254696:T:TA | donor_gain | 1.0000 |
| 6:93254697:C:A | donor_gain | 1.0000 |
| 6:93254792:CCACC:C | acceptor_gain | 1.0000 |
| 6:93254793:CACC:C | acceptor_gain | 1.0000 |
| 6:93254793:CACCC:C | acceptor_gain | 1.0000 |
| 6:93254795:CC:C | acceptor_gain | 1.0000 |
| 6:93254796:CCTG:C | acceptor_loss | 1.0000 |
| 6:93254796:CCTGT:C | acceptor_gain | 1.0000 |
| 6:93254797:C:A | acceptor_loss | 1.0000 |
| 6:93254798:T:A | acceptor_loss | 1.0000 |
| 6:93255826:A:AC | donor_gain | 1.0000 |
| 6:93255827:C:CC | donor_gain | 1.0000 |
| 6:93255827:CAGTA:C | donor_gain | 1.0000 |
| 6:93256033:TGTTT:T | acceptor_gain | 1.0000 |
| 6:93257456:ACTT:A | donor_loss | 1.0000 |
| 6:93257457:CTT:C | donor_loss | 1.0000 |
| 6:93257458:TTACC:T | donor_loss | 1.0000 |
| 6:93257459:TACCC:T | donor_loss | 1.0000 |
| 6:93257460:A:AC | donor_gain | 1.0000 |
| 6:93257460:A:C | donor_loss | 1.0000 |
| 6:93257460:AC:A | donor_gain | 1.0000 |
AlphaMissense
6592 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 6:93245385:A:G | L932P | 1.000 |
| 6:93245389:A:G | W931R | 1.000 |
| 6:93245389:A:T | W931R | 1.000 |
| 6:93246878:C:A | R880S | 1.000 |
| 6:93246878:C:G | R880S | 1.000 |
| 6:93246901:A:G | W873R | 1.000 |
| 6:93246901:A:T | W873R | 1.000 |
| 6:93246954:A:G | L855S | 1.000 |
| 6:93254667:A:G | W838R | 1.000 |
| 6:93254667:A:T | W838R | 1.000 |
| 6:93254670:A:C | Y837D | 1.000 |
| 6:93254672:G:T | P836H | 1.000 |
| 6:93254698:C:A | W827C | 1.000 |
| 6:93254698:C:G | W827C | 1.000 |
| 6:93254700:A:G | W827R | 1.000 |
| 6:93254700:A:T | W827R | 1.000 |
| 6:93254711:C:T | G823E | 1.000 |
| 6:93254712:C:G | G823R | 1.000 |
| 6:93254712:C:T | G823R | 1.000 |
| 6:93254721:A:G | W820R | 1.000 |
| 6:93254721:A:T | W820R | 1.000 |
| 6:93254727:C:G | D818H | 1.000 |
| 6:93254728:A:C | S817R | 1.000 |
| 6:93254728:A:T | S817R | 1.000 |
| 6:93254730:T:G | S817R | 1.000 |
| 6:93254740:G:C | F813L | 1.000 |
| 6:93254740:G:T | F813L | 1.000 |
| 6:93254742:A:G | F813L | 1.000 |
| 6:93254773:C:A | W802C | 1.000 |
| 6:93254773:C:G | W802C | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000009611 (6:93327753 A>C), RS1000010535 (6:93379448 T>A,C), RS1000014757 (6:93349619 C>A,T), RS1000014840 (6:93336656 C>T), RS1000025662 (6:93293252 T>G), RS1000041780 (6:93242412 G>T), RS1000041843 (6:93256990 A>G,T), RS1000046362 (6:93330483 T>C), RS1000049276 (6:93420067 T>C), RS1000060378 (6:93349385 C>G,T), RS1000094023 (6:93299980 G>C), RS1000094269 (6:93287401 G>A), RS1000098887 (6:93414591 T>C), RS1000109514 (6:93246710 A>G), RS1000129487 (6:93353889 G>C)
Disease associations
OMIM: gene MIM:602190 | disease phenotypes:
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| neurodevelopmental disorder | Moderate | Autosomal dominant |
Mondo (2): intellectual disability (MONDO:0001071), neurodevelopmental disorder (MONDO:0700092)
Orphanet (1): NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
19 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001066_4 | Dialysis-related mortality | 1.000000e-06 |
| GCST001325_6 | Response to hepatitis C treatment | 7.000000e-06 |
| GCST002345_8 | Response to cytadine analogues (cytosine arabinoside) | 8.000000e-06 |
| GCST002597_3 | Laryngeal squamous cell carcinoma | 7.000000e-07 |
| GCST002875_8 | Diisocyanate-induced asthma | 7.000000e-06 |
| GCST003989_4 | Chin dimples | 4.000000e-08 |
| GCST005023_20 | Initial pursuit acceleration | 8.000000e-06 |
| GCST007324_44 | Adventurousness | 4.000000e-08 |
| GCST007327_44 | Smoking status (ever vs never smokers) | 1.000000e-08 |
| GCST007490_15 | Anthropometric traits (multi-trait analysis) | 7.000000e-10 |
| GCST008161_100 | Waist circumference adjusted for body mass index | 4.000000e-07 |
| GCST008810_62 | Smoking initiation (ever regular vs never regular) | 2.000000e-09 |
| GCST010796_2684 | Electrocardiogram morphology (amplitude at temporal datapoints) | 9.000000e-10 |
| GCST010796_2685 | Electrocardiogram morphology (amplitude at temporal datapoints) | 5.000000e-10 |
| GCST010796_2686 | Electrocardiogram morphology (amplitude at temporal datapoints) | 2.000000e-08 |
| GCST010796_2687 | Electrocardiogram morphology (amplitude at temporal datapoints) | 1.000000e-10 |
| GCST010988_369 | Adult body size | 2.000000e-08 |
| GCST012244_5 | Childhood asthma exacerbations in long-acting beta2-agonist treatment | 3.000000e-06 |
| GCST90007005_5 | Gut microbiota relative abundance (Eubacterium belonging to family Erysipelotrichaceae) | 1.000000e-06 |
EFO canonical traits (10, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006995 | response to diisocyanate |
| EFO:0008434 | initial pursuit acceleration |
| EFO:0008579 | risk-taking behaviour |
| EFO:0004318 | smoking behavior |
| EFO:0004324 | body weights and measures |
| EFO:0007789 | BMI-adjusted waist circumference |
| EFO:0005670 | smoking initiation |
| EFO:0004327 | electrocardiography |
| EFO:0007614 | asthma exacerbation measurement |
| EFO:0007874 | gut microbiome measurement |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
| D065886 | Neurodevelopmental Disorders | F03.625 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2363043 (PROTEIN FAMILY), CHEMBL4602 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
29 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 373,602 (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 |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1336 | SORAFENIB | 4 | 86,060 |
| CHEMBL24828 | VANDETANIB | 4 | 42,230 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,395 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL553 | ERLOTINIB | 4 | 108,300 |
| CHEMBL576982 | QUIZARTINIB | 4 | 4,432 |
| CHEMBL601719 | CRIZOTINIB | 4 | 14,403 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL31965 | CANERTINIB | 3 | 8,083 |
| CHEMBL3544983 | TESEVATINIB | 3 | 2,819 |
| CHEMBL377300 | BRIVANIB | 3 | 1,721 |
| CHEMBL491473 | CEDIRANIB | 3 | 9,098 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL103667 | DORAMAPIMOD | 2 | 1,681 |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL1738757 | REBASTINIB | 2 | 1,478 |
| CHEMBL3039525 | GOLVATINIB | 2 | 535 |
| CHEMBL3991932 | PEXMETINIB | 2 | 409 |
| CHEMBL402548 | DANUSERTIB | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL495727 | AT-9283 | 2 | |
| CHEMBL575448 | BMS-754807 | 2 | |
| CHEMBL1908397 | KW-2449 | 1 | |
| CHEMBL259084 | MLN-8054 | 1 | |
| CHEMBL3544932 | TAK-901 | 1 | |
| CHEMBL3545085 | XL-228 | 1 | |
| CHEMBL574738 | AST-487 | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
1 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs78132896 | Toxicity | 3 | warfarin | Hemorrhage |
PharmGKB variants
2 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs78132896 | EPHA7 | 3 | 1.88 | 1 | warfarin |
| rs114504854 | EPHA7 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: catalytic receptor — Type XIII RTKs: Ephrin receptor family
Most potent curated ligand interactions (4 total), top 4:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| compound 8h [PMID: 21561767] | Inhibition | 8.38 | pIC50 |
| DDR1/2 inhibitor 5n | Inhibition | 6.7 | pKd |
| compound 66 [PMID: 19788238] | Inhibition | 5.95 | pIC50 |
| compound 20 [PMID: 23489211] | Inhibition | 5.68 | pIC50 |
Binding affinities (BindingDB)
17 measured of 17 human assays (17 total across all organisms); most potent 17 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | KD | 0.37 nM | |
| Staurosporine | KD | 1.7 nM | |
| 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole | KD | 9.8 nM | |
| 4-[4-(4-fluorophenyl)-2-(4-methanesulfinylphenyl)-1H-imidazol-5-yl]pyridine | KD | 12 nM | |
| N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine | KD | 150 nM | |
| AMG 706 | KD | 300 nM | |
| 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid | KD | 300 nM | |
| 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide | KD | 370 nM | |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea | KD | 450 nM | |
| ERLOTINIB HYDROCHLORIDE | KD | 1200 nM | |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM | |
| CI-1033 | KD | 1700 nM | |
| GEFITINIB | IC50 | 2300 nM | US-9416123: Kinase modulators for the treatment of cancer |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM | |
| 1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | KD | 3100 nM | |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM | |
| 1-methyl-5-[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]pyridin-4-yl]oxy-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine | KD | 4500 nM |
ChEMBL bioactivities
78 potent at pChembl≥5 of 80 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.75 | IC50 | 1.77 | nM | CHEMBL5423601 |
| 8.60 | Kd | 2.5 | nM | FORETINIB |
| 8.38 | IC50 | 4.2 | nM | CHEMBL1784637 |
| 8.30 | Kd | 5 | nM | FORETINIB |
| 8.10 | Kd | 8 | nM | AT-9283 |
| 7.80 | Kd | 16 | nM | CHEMBL3688339 |
| 7.77 | Kd | 17 | nM | XL-228 |
| 7.66 | Kd | 22 | nM | TESEVATINIB |
| 7.41 | IC50 | 39.2 | nM | STAUROSPORINE |
| 7.41 | Kd | 39 | nM | R-406 |
| 7.40 | Kd | 40 | nM | DANUSERTIB |
| 7.34 | IC50 | 45.5 | nM | STAUROSPORINE |
| 7.25 | IC50 | 56.3 | nM | STAUROSPORINE |
| 7.11 | Kd | 77 | nM | GOLVATINIB |
| 7.06 | IC50 | 88 | nM | REBASTINIB |
| 6.99 | Kd | 102 | nM | R-406 |
| 6.96 | Kd | 110 | nM | LINIFANIB |
| 6.84 | IC50 | 143 | nM | CHEMBL4798527 |
| 6.79 | IC50 | 162 | nM | CHEMBL5195469 |
| 6.72 | IC50 | 190 | nM | CHEMBL4281823 |
| 6.70 | Kd | 200 | nM | CHEMBL4168305 |
| 6.70 | IC50 | 199 | nM | CHEMBL4793380 |
| 6.70 | Kd | 200 | nM | TAE-684 |
| 6.66 | Kd | 220 | nM | DORAMAPIMOD |
| 6.58 | Kd | 260 | nM | LESTAURTINIB |
| 6.41 | Kd | 390 | nM | KW-2449 |
| 6.33 | Kd | 470 | nM | CRIZOTINIB |
| 6.21 | Kd | 615 | nM | TAK-901 |
| 6.21 | Kd | 620 | nM | CEDIRANIB |
| 6.20 | Kd | 630 | nM | STAUROSPORINE |
| 6.18 | IC50 | 665 | nM | CHEMBL3715238 |
| 6.17 | Kd | 670 | nM | SORAFENIB |
| 6.16 | Kd | 690 | nM | STAUROSPORINE |
| 6.15 | Kd | 710 | nM | SUNITINIB |
| 6.12 | Kd | 766 | nM | CHEMBL4465866 |
| 6.07 | Kd | 860 | nM | DORAMAPIMOD |
| 6.05 | Kd | 887 | nM | CHEMBL4576489 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 6.00 | Kd | 1000 | nM | MLN-8054 |
| 5.96 | Kd | 1100 | nM | AST-487 |
| 5.95 | IC50 | 1118 | nM | CHEMBL566515 |
| 5.93 | Kd | 1182 | nM | CHEMBL5653589 |
| 5.92 | Kd | 1190 | nM | CANERTINIB |
| 5.85 | Kd | 1400 | nM | ERLOTINIB |
| 5.83 | ED50 | 1493 | nM | CHEMBL5653589 |
| 5.82 | Kd | 1500 | nM | CANERTINIB |
| 5.82 | Kd | 1500 | nM | SU-014813 |
| 5.77 | Kd | 1700 | nM | BRIVANIB |
PubChem BioAssay actives
74 with measured affinity, of 937 total; 49 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 |
|---|---|---|---|---|
| N-[3-cyclopropyl-5-[(4-methylpiperazin-1-yl)methyl]phenyl]-5-methyl-18-oxo-9-oxa-17,23,25,26-tetrazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide | 2014046: Inhibition of EphA7 (unknown origin) | ic50 | 0.0018 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 624953: Binding constant for EPHA7 kinase domain | kd | 0.0025 | uM |
| 5-[2-[5-[[4-[[4-(2-hydroxyethyl)piperazin-1-yl]methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]ethynyl]-N,1-dimethylimidazole-2-carboxamide | 601673: Inhibition of human EPHA7 using poly[Glu:Tyr] peptide substrate by Hotspot assay | ic50 | 0.0042 | uM |
| 1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0080 | uM |
| 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0160 | uM |
| 4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0170 | uM |
| 7-[[(3aS,6aR)-2-methyl-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-5-yl]methoxy]-N-(3,4-dichloro-2-fluorophenyl)-6-methoxyquinazolin-4-amine | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0220 | uM |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | 624953: Binding constant for EPHA7 kinase domain | kd | 0.0390 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 1715365: Inhibition of human EPHA7 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay | ic50 | 0.0392 | uM |
| N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-d]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0400 | uM |
| 1-N’-[2-fluoro-4-[[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]-4-pyridinyl]oxy]phenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0770 | uM |
| 4-[4-[(3-tert-butyl-1-quinolin-6-ylpyrazol-5-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | 2168202: Inhibition of human wild type EPHA7 using PolyEY as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | ic50 | 0.0880 | uM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | 624953: Binding constant for EPHA7 kinase domain | kd | 0.1100 | uM |
| N-[3-[2-[4-amino-1-(4-hydroxycyclohexyl)pyrazolo[3,4-d]pyrimidin-3-yl]ethynyl]-4-methylphenyl]-4-methyl-3-(trifluoromethyl)benzamide | 1734783: Inhibition of human recombinant EPHA7 (613 to 909 residues) using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC incubated for 40 mins in presence of [gamma33P-ATP] by radiometric scintillation counting analysis | ic50 | 0.1430 | uM |
| 5,18-dimethyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-14-oxo-9-oxa-15,18,23,25,26-pentazatetracyclo[17.5.2.14,8.022,25]heptacosa-1(24),4,6,8(27),19(26),20,22-heptaen-2-yne-6-carboxamide | 1908202: Inhibition of human wild type partial length EphA7 (Y608 to S912 residues) expressed in bacterial expression system by Kinomescan method | ic50 | 0.1620 | uM |
| 1-[5-(4-amino-7-ethylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-(trifluoromethoxy)phenyl]ethanone | 1415175: Inhibition of recombinant human EphA7 (613 to 909 residues) using KTFCGTPEYLAPE as substrate after 40 mins in presence of [gamma-33P]-ATP by scintillation counting analysis | ic50 | 0.1900 | uM |
| 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-(6,7,8,9-tetrahydropyrimido[5,4-b][1,4]oxazepin-4-ylamino)phenyl]urea | 1735603: Inhibition of recombinant human EphA7 (613 to 909 residues) using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate incubated for 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay | ic50 | 0.1990 | uM |
| 3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-ylbenzamide | 1356732: Binding affinity to human EPHA7 | kd | 0.2000 | uM |
| 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine | 624953: Binding constant for EPHA7 kinase domain | kd | 0.2000 | uM |
| 1-[3-tert-butyl-1-(4-methylphenyl)pyrazol-5-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 256585: Average Binding Constant for EPHA7; NA=Not Active at 10 uM | kd | 0.2200 | uM |
| (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one | 507925: Binding affinity to EPHA7 | kd | 0.2600 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624953: Binding constant for EPHA7 kinase domain | kd | 0.3900 | uM |
| Crizotinib | 624953: Binding constant for EPHA7 kinase domain | kd | 0.4700 | uM |
| 5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.6150 | uM |
| 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline | 624953: Binding constant for EPHA7 kinase domain | kd | 0.6200 | uM |
| 5-[1-(cyclopropylmethyl)-5-[(1R,5S)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl]pyrazol-3-yl]-3-(trifluoromethyl)pyridin-2-amine | 1491957: Inhibition of recombinant GST-tagged human EphA7 cytoplasmic domain expressed in baculovirus expression system by FRET assay | ic50 | 0.6650 | uM |
| Sorafenib | 256585: Average Binding Constant for EPHA7; NA=Not Active at 10 uM | kd | 0.6700 | uM |
| Sunitinib | 256585: Average Binding Constant for EPHA7; NA=Not Active at 10 uM | kd | 0.7100 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526215: Binding affinity to recombinant N-terminal His-FLAG-GST-tagged EPHA7 (unknown origin) ( 595 to 998 residues) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.7660 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526215: Binding affinity to recombinant N-terminal His-FLAG-GST-tagged EPHA7 (unknown origin) ( 595 to 998 residues) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.8870 | uM |
| 4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid | 435286: Binding constant for EPHA7 kinase domain | kd | 1.0000 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435286: Binding constant for EPHA7 kinase domain | kd | 1.1000 | uM |
| 7-(5-hydroxy-2-methylphenyl)-6-(2-methoxyphenyl)-4-methylpurino[7,8-a]imidazole-1,3-dione | 441390: Inhibition of EphA7 by [gamma33-P]ATP based assay | ic50 | 1.1180 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2147761: Binding affinity to human EPHA7 incubated for 45 mins by Kinobead based pull down assay | kd | 1.1825 | uM |
| N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 1.1900 | uM |
| Erlotinib | 435286: Binding constant for EPHA7 kinase domain | kd | 1.4000 | uM |
| 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | 624953: Binding constant for EPHA7 kinase domain | kd | 1.5000 | uM |
| (2R)-1-[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol | 624953: Binding constant for EPHA7 kinase domain | kd | 1.7000 | uM |
| (2S)-2-[[(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 728715: Displacement of ephrin-A1-Fc from EphA7 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | ic50 | 2.1000 | uM |
| Vandetanib | 435286: Binding constant for EPHA7 kinase domain | kd | 2.4000 | uM |
| (2S)-2-[[(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1H-indol-3-yl)propanoic acid | 1260965: Displacement of biotinylated ephrin-A1-Fc from EphA7 (unknown origin) preincubated for 1 hr followed by biotinylated-ephrin-A1-Fc addition measured after 4 hrs by ELISA | ic50 | 2.5000 | uM |
| Gilteritinib | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 2.9800 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435286: Binding constant for EPHA7 kinase domain | kd | 3.1000 | uM |
| 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[2-(5-hydroxy-1H-indole-2-carbonyl)-1-benzofuran-5-yl]urea | 1691312: Inhibition of human EPHA7 incubated for 30 mins by Kinobead based assay | ec50 | 3.2550 | uM |
| 1-[3-tert-butyl-1-(4-methylphenyl)pyrazol-5-yl]-3-[[5-fluoro-2-[1-(2-hydroxyethyl)indazol-5-yl]oxyphenyl]methyl]urea | 1424991: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.3120 | uM |
| Quizartinib | 624953: Binding constant for EPHA7 kinase domain | kd | 3.7000 | uM |
| (2S)-1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methylpyrrolidine-2-carboxamide | 2167418: Binding affinity to EPHA7 (unknown origin) by phage based competition assay | kd | 5.0000 | uM |
| Fedratinib | 624953: Binding constant for EPHA7 kinase domain | kd | 6.5000 | uM |
| 5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride | 624953: Binding constant for EPHA7 kinase domain | kd | 6.7000 | uM |
CTD chemical–gene interactions
36 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, decreases expression, affects expression, decreases methylation, increases expression | 7 |
| trichostatin A | affects cotreatment, decreases expression, affects expression, decreases reaction, increases expression | 4 |
| Nickel | decreases expression, decreases reaction, affects expression | 3 |
| entinostat | affects cotreatment, increases expression | 2 |
| ponatinib | decreases activity | 2 |
| Panobinostat | affects cotreatment, increases expression | 2 |
| Benzo(a)pyrene | increases methylation, affects methylation, decreases expression | 2 |
| Estradiol | affects cotreatment, decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| methylmercuric chloride | decreases expression | 1 |
| terbufos | increases methylation | 1 |
| sulforaphane | decreases expression | 1 |
| pentanal | decreases expression | 1 |
| polyhexamethyleneguanidine | affects expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression, decreases expression | 1 |
| belinostat | increases expression | 1 |
| abrine | decreases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression, decreases expression | 1 |
| Sunitinib | increases expression | 1 |
| Arsenates | affects cotreatment, increases expression | 1 |
| Atrazine | affects cotreatment, increases expression | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| Doxorubicin | decreases expression | 1 |
| Fonofos | increases methylation | 1 |
| Parathion | increases methylation | 1 |
| Progesterone | affects cotreatment, decreases expression | 1 |
| Silver | decreases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Triclosan | decreases expression | 1 |
ChEMBL screening assays
231 unique, capped per target: 231 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1024911 | Binding | Binding affinity to human EPHA7 at 10 uM relative to control | Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. — J Med Chem |
Clinical trials (associated diseases)
390 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| 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, |
| NCT05657860 | PHASE4 | COMPLETED | Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome |
| NCT05744479 | PHASE4 | RECRUITING | Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability |
| NCT06107829 | PHASE4 | WITHDRAWN | Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities |
| NCT06997198 | PHASE4 | NOT_YET_RECRUITING | Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities |
| 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 |
| NCT02270736 | PHASE3 | COMPLETED | Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability |
| 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 |
| NCT02304302 | PHASE2 | COMPLETED | Down Syndrome Memantine Follow-up Study |
| NCT03862950 | PHASE2 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome (Met) |
| NCT04529226 | PHASE2 | UNKNOWN | Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis |
| NCT04821856 | PHASE2 | COMPLETED | Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability |
| 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 |
| NCT05273320 | PHASE1 | COMPLETED | Clinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities |
| NCT05301361 | PHASE1 | ENROLLING_BY_INVITATION | Sensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities |
| NCT06016764 | PHASE1 | COMPLETED | Use of MRI and cTBS for Catatonia in Autism |
| NCT06586827 | PHASE1 | COMPLETED | Impact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD |
| NCT07531940 | PHASE1 | NOT_YET_RECRUITING | Escalating Doses of Memantine in Down Syndrome (MEDS-123) |
| NCT01783041 | PHASE2/PHASE3 | COMPLETED | Effect of Early L-Carnitine Supplementation on Neurodevelopmental Outcomes in Very Preterm Infants |
| NCT05767385 | PHASE2/PHASE3 | RECRUITING | Fetal Cerebrovascular Autoregulation in Congenital Heart Disease and Association With Neonatal Neurobehavior |
| NCT05675098 | EARLY_PHASE1 | NOT_YET_RECRUITING | Central Nervous System Stimulants and Physical Function in Children With Cerebral Palsy |
| NCT00783783 | Not specified | COMPLETED | CYP2D6 Pharmacogenetics in Risperidone-Treated Children |
| NCT01778504 | Not specified | RECRUITING | Studying Childhood-onset Behavioral, Psychiatric, and Developmental Disorders |
| NCT01850784 | Not specified | UNKNOWN | High Energy Formula Feeding in Infants With Congenital Heart Disease |
| NCT01922791 | Not specified | COMPLETED | Nutrition and Pregnancy Intervention Study |
| NCT01942525 | Not specified | UNKNOWN | Influence of Intrauterine Growth Restriction on Amplitude-integrated EEG in Preterm Infants |
| NCT02003170 | Not specified | COMPLETED | Etiology and Early Diagnosis of Neurodevelopmental Disorders |
| NCT02118649 | Not specified | ACTIVE_NOT_RECRUITING | Enhancing Behavior and Brain Response to Visual Targets Using a Computer Game |
| NCT02557191 | Not specified | TERMINATED | Biomarkers, Neurodevelopment and Preterm Infants |
| NCT02690675 | Not specified | COMPLETED | Iron Supplement Effect on Child Development |
| NCT02694003 | Not specified | COMPLETED | Better Nights, Better Days for Children With Neurodevelopment Disorders |
| NCT02792894 | Not specified | COMPLETED | Family Networks (FaNs) for Children With Developmental Disorders and Delays |
Related Atlas pages
- Associated diseases: neurodevelopmental disorder
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): chronic hepatitis C virus infection, laryngeal squamous cell carcinoma