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Target Report Card

Target Name and Classification

Target ID CHEMBL1936
Target Type SINGLE PROTEIN
Preferred Name Stem cell growth factor receptor
Synonyms CD_antigen=CD117 | KIT | Mast/stem cell growth factor receptor Kit | PBT | Piebald trait protein | Proto-oncogene c-Kit | SCFR | SCFR | Tyrosine-protein kinase Kit | p145 c-kit | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase pdgfr family

Target Components

Component Description Relationship Accession
Mast/stem cell growth factor receptor Kit SINGLE PROTEIN P10721

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111428 VEGF-receptor 2 and stem cell growth factor receptor (KDR and KIT) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1421 DASATINIB Stem cell growth factor receptor inhibitor 4 DailyMed
CHEMBL1567 SUNITINIB MALATE Stem cell growth factor receptor inhibitor 4 DailyMed
CHEMBL1642 IMATINIB MESYLATE Stem cell growth factor receptor inhibitor 4 DailyMed
CHEMBL1200485 SORAFENIB TOSYLATE Stem cell growth factor receptor inhibitor 4 FDA
CHEMBL1201733 PAZOPANIB HYDROCHLORIDE Stem cell growth factor receptor inhibitor 4 DailyMed
CHEMBL1946170 REGORAFENIB Stem cell growth factor receptor inhibitor 4 Expert
CHEMBL276711 SEMAXANIB Stem cell growth factor receptor inhibitor 3 PubMed PubMed
CHEMBL101253 VATALANIB Stem cell growth factor receptor inhibitor 3 PubMed PubMed
CHEMBL491473 CEDIRANIB Stem cell growth factor receptor inhibitor 3 PubMed
CHEMBL522892 DOVITINIB Stem cell growth factor receptor inhibitor 3 PubMed
CHEMBL572881 MOTESANIB Stem cell growth factor receptor inhibitor 3 PubMed
CHEMBL576982 QUIZARTINIB Stem cell growth factor receptor inhibitor 3 PubMed PubMed
CHEMBL608533 MIDOSTAURIN Stem cell growth factor receptor inhibitor 3 PubMed PubMed
CHEMBL1908391 MASITINIB Stem cell growth factor receptor inhibitor 3 Other PubMed PubMed
CHEMBL3545026 Famitinib Stem cell growth factor receptor inhibitor 3 ClinicalTrials DOI PubMed
CHEMBL3545158 PLX-3397 Stem cell growth factor receptor inhibitor 3 PubMed PubMed
CHEMBL124660 TANDUTINIB Stem cell growth factor receptor inhibitor 2 Other PubMed PubMed
CHEMBL482968 ENMD-2076 Stem cell growth factor receptor inhibitor 2 Other PubMed PubMed
CHEMBL1230609 FORETINIB Stem cell growth factor receptor inhibitor 2 Other PubMed
CHEMBL1721885 SU-014813 Stem cell growth factor receptor inhibitor 2 PubMed
CHEMBL2079588 TELATINIB Stem cell growth factor receptor inhibitor 2 PubMed PubMed
CHEMBL2103851 AMUVATINIB Stem cell growth factor receptor inhibitor 2 Other PubMed PubMed
CHEMBL3545021 Anlotinib Stem cell growth factor receptor inhibitor 2 ClinicalTrials Other
CHEMBL3545160 SU-14813 Stem cell growth factor receptor inhibitor 2 PubMed
CHEMBL3545285 XL-999 Stem cell growth factor receptor inhibitor 2 DOI Other PubMed
CHEMBL3545402 XL-820 Stem cell growth factor receptor inhibitor 2 Other Other
CHEMBL1614710 OSI-930 Stem cell growth factor receptor inhibitor 1 PubMed PubMed
CHEMBL3545427 CM-082 Stem cell growth factor receptor inhibitor 1 Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000157404
Ensembl ENSG00000157404
GO Cellular Component GO:0001669 (acrosomal vesicle)
GO:0005615 (extracellular space)
GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005911 (cell-cell junction)
GO:0009897 (external side of plasma membrane)
GO:0009898 (cytoplasmic side of plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0042629 (mast cell granule)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0002020 (protease binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0005020 (stem cell factor receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019955 (cytokine binding)
GO:0042803 (protein homodimerization activity)
GO:0046872 (metal ion binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0000187 (activation of MAPK activity)
GO:0001541 (ovarian follicle development)
GO:0002318 (myeloid progenitor cell differentiation)
GO:0002320 (lymphoid progenitor cell differentiation)
GO:0002327 (immature B cell differentiation)
GO:0002371 (dendritic cell cytokine production)
GO:0002551 (mast cell chemotaxis)
GO:0002573 (myeloid leukocyte differentiation)
GO:0006468 (protein phosphorylation)
GO:0006687 (glycosphingolipid metabolic process)
GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007283 (spermatogenesis)
GO:0007286 (spermatid development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008354 (germ cell migration)
GO:0008360 (regulation of cell shape)
GO:0008542 (visual learning)
GO:0008584 (male gonad development)
GO:0009314 (response to radiation)
GO:0010628 (positive regulation of gene expression)
GO:0010863 (positive regulation of phospholipase C activity)
GO:0014066 (regulation of phosphatidylinositol 3-kinase signaling)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0019221 (cytokine-mediated signaling pathway)
GO:0019827 (stem cell population maintenance)
GO:0030032 (lamellipodium assembly)
GO:0030097 (hemopoiesis)
GO:0030217 (T cell differentiation)
GO:0030218 (erythrocyte differentiation)
GO:0030318 (melanocyte differentiation)
GO:0030335 (positive regulation of cell migration)
GO:0031274 (positive regulation of pseudopodium assembly)
GO:0031532 (actin cytoskeleton reorganization)
GO:0032762 (mast cell cytokine production)
GO:0035019 (somatic stem cell population maintenance)
GO:0035162 (embryonic hemopoiesis)
GO:0035234 (ectopic germ cell programmed cell death)
GO:0035556 (intracellular signal transduction)
GO:0035701 (hematopoietic stem cell migration)
GO:0035855 (megakaryocyte development)
GO:0038093 (Fc receptor signaling pathway)
GO:0038109 (Kit signaling pathway)
GO:0038162 (erythropoietin-mediated signaling pathway)
GO:0042127 (regulation of cell proliferation)
GO:0042511 (positive regulation of tyrosine phosphorylation of Stat1 protein)
GO:0042517 (positive regulation of tyrosine phosphorylation of Stat3 protein)
GO:0042523 (positive regulation of tyrosine phosphorylation of Stat5 protein)
GO:0043069 (negative regulation of programmed cell death)
GO:0043303 (mast cell degranulation)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0043410 (positive regulation of MAPK cascade)
GO:0043473 (pigmentation)
GO:0043547 (positive regulation of GTPase activity)
GO:0043552 (positive regulation of phosphatidylinositol 3-kinase activity)
GO:0045747 (positive regulation of Notch signaling pathway)
GO:0046427 (positive regulation of JAK-STAT cascade)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048066 (developmental pigmentation)
GO:0048070 (regulation of developmental pigmentation)
GO:0048103 (somatic stem cell division)
GO:0048170 (positive regulation of long-term neuronal synaptic plasticity)
GO:0048565 (digestive tract development)
GO:0048863 (stem cell differentiation)
GO:0050673 (epithelial cell proliferation)
GO:0050910 (detection of mechanical stimulus involved in sensory perception of sound)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0060326 (cell chemotaxis)
GO:0060374 (mast cell differentiation)
GO:0070662 (mast cell proliferation)
GO:0097067 (cellular response to thyroid hormone stimulus)
GO:0097324 (melanocyte migration)
GO:0097326 (melanocyte adhesion)
GO:1905065 (positive regulation of vascular smooth muscle cell differentiation)
Wikipedia CD117

Target Cross References - Protein

canSAR P10721
CGD Gastrointestinal stromal tumor
Human Protein Atlas ENSG00000157404
IntAct P10721
Guide to Pharmacology 1805
Open Targets ENSG00000157404
PharmGKB PA30128
Pharos P10721 (Tclin)
Reactome R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-1433557 (Signaling by SCF-KIT.)
R-HSA-1433559 (Regulation of KIT signaling.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8866910 (TFAP2 (AP-2) family regulates transcription of growth factors and their receptors.)
UniProt B5A956 D5LXN2 D5M931 F5H8F8 P10721 Q6IQ28 Q99662 Q9UM99

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR001824 (Tyr_kinase_rcpt_3_CS.)
IPR003598 (Ig_sub2.)
IPR003599 (Ig_sub.)
IPR007110 (Ig-like_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom.)
IPR013151 (Immunoglobulin.)
IPR013783 (Ig-like_fold.)
IPR016243 (Tyr_kinase_CSF1/PDGF_rcpt.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR027263 (SCGF_receptor.)
Pfam PF00047 (ig)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1PKG 1T45 1T46 2E9W 2EC8 2IUH 2VIF 3G0E 3G0F 4HVS 4K94 4K9E 4PGZ 4U0I
CREDO 1PKG 1T45 1T46 2E9W 2EC8 2IUH 2VIF 3G0E 3G0F 4HVS 4K94 4K9E 4PGZ 4U0I
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