Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	1	976	4q12	KIT	KIT proto-oncogene, receptor tyrosine kinase
Mouse	1	979	5 39.55 cM	Kit	KIT proto-oncogene receptor tyrosine kinase
Rat	-	978	14p11	Kit	KIT proto-oncogene receptor tyrosine kinase

Previous and Unofficial Names

CD117 | C-Kit | PBT | stem cell growth factor receptor | piebald trait | c-kit receptor tyrosine kinase | mast/stem cell growth factor receptor | p145 c-kit | Proto-oncogene c-Kit | Steel Factor Receptor | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog | kit oncogene | KIT proto-oncogene receptor tyrosine kinase

Database Links
Alphafold	P10721 (Hs), P05532 (Mm)
BRENDA	2.7.10.1
CATH/Gene3D	2.60.40.10
ChEMBL Target	CHEMBL1936 (Hs), CHEMBL2034798 (Mm)
DrugBank Target	P10721 (Hs)
Ensembl Gene	ENSG00000157404 (Hs), ENSMUSG00000005672 (Mm), ENSRNOG00000002227 (Rn)
Entrez Gene	3815 (Hs), 16590 (Mm), 64030 (Rn)
Human Protein Atlas	ENSG00000157404 (Hs)
KEGG Enzyme	2.7.10.1
KEGG Gene	hsa:3815 (Hs), mmu:16590 (Mm), rno:64030 (Rn)
OMIM	164920 (Hs)
Orphanet	ORPHA122862 (Hs)
Pharos	P10721 (Hs)
RefSeq Nucleotide	NM_000222 (Hs), NM_001122733 (Mm), NM_022264 (Rn)
RefSeq Protein	NP_000213 (Hs), NP_066922 (Mm), NP_001116205 (Mm), NP_071600 (Rn)
SynPHARM	81286 (in complex with sunitinib) 81225 (in complex with sunitinib)
UniProtKB	P10721 (Hs), P05532 (Mm)
Wikipedia	KIT (Hs)

Selected 3D Structures
	Description:  Crystal structure of the extracellular domain of the receptor tyrosine kinase, Kit PDB Id:  2EC8 Resolution:  3.0Å Species:  Human References:  70
	Description:  KIT kinase domain in complex with sunitinib PDB Id:  3G0E Ligand:  sunitinib Resolution:  1.6Å Species:  Human References:  18

Enzyme Reaction
EC Number: 2.7.10.1

Natural/Endogenous Ligands
stem cell factor {Sp: Human}

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference sunitinib Hs Inhibition 9.4 pKd 12 ⤷ pKd 9.4 (Kd 3.7x10-10 M) [12] AC710 Hs Inhibition 9.0 pKd 40 ⤷ pKd 9.0 (Kd 1x10-9 M) [40] compound 6li [Chan et al., 2022] Hs Inhibition 8.6 pKd 9 ⤷ pKd 8.6 (Kd 2.6x10-9 M) [9] quizartinib Hs Inhibition 8.3 pKd 10 ⤷ pKd 8.3 (Kd 4.8x10-9 M) [10] masitinib Hs Inhibition 8.1 pKd 12 ⤷ pKd 8.1 (Kd 8.1x10-9 M) [12] RG-1530 Hs Inhibition 7.6 pKd 59 ⤷ pKd 7.6 (Kd 2.6x10-8 M) [59] crenolanib Hs Inhibition 7.1 pKd 30 ⤷ pKd 7.1 (Kd 7.8x10-8 M) [30] BPR1R024 Hs Inhibition 9.0 pIC50 38 ⤷ pIC50 9.0 (IC50 1.1x10-9 M) [38] famitinib Hs Inhibition 8.7 pIC50 11 ⤷ pIC50 8.7 (IC50 2x10-9 M) [11] dovitinib Hs Inhibition 8.5 – 8.7 pIC50 52,60 ⤷ pIC50 8.5 – 8.7 (IC50 3x10-9 – 2x10-9 M) [52,60] cediranib Hs Inhibition 8.5 pIC50 62 ⤷ pIC50 8.5 (IC50 3x10-9 M) [62] CHMFL-KIT-64 Hs Inhibition 8.4 pIC50 67 ⤷ pIC50 8.4 (IC50 4x10-9 M) [67] Description: In a biochemical assay. ibcasertib Hs Inhibition 8.4 pIC50 73 ⤷ pIC50 8.4 (IC50 4x10-9 M) [73] Description: Inhibition in a biochemical assay. elenestinib Hs Inhibition >8.4 pIC50 35 ⤷ pIC50 >8.4 (IC50 <4.5x10-9 M) [35] Description: Biochemical inhibition assay, using KITD816V compound 7k [PMID: 23521020] Hs Inhibition 8.3 pIC50 20 ⤷ pIC50 8.3 (IC50 4.89x10-9 M) [20] JNJ-28312141 Hs Inhibition 8.3 pIC50 42 ⤷ pIC50 8.3 (IC50 5x10-9 M) [42] sitravatinib Hs Inhibition 8.2 pIC50 48 ⤷ pIC50 8.2 (IC50 6x10-9 M) [48] Description: In a biochemical enzyme activity assay. risvodetinib Hs Inhibition 8.1 pIC50 64 ⤷ pIC50 8.1 (IC50 7.8x10-9 M) [64] henatinib Hs Inhibition 8.1 pIC50 11 ⤷ pIC50 8.1 (IC50 8x10-9 M) [11] SU11652 Hs Inhibition 8.0 pIC50 16 ⤷ pIC50 8.0 (IC50 1x10-8 M) [16] KBP-7018 Hs Inhibition 8.0 pIC50 31 ⤷ pIC50 8.0 (IC50 1x10-8 M) [31] compound 8h [PMID: 22765894] Hs Inhibition 8.0 pIC50 36 ⤷ pIC50 8.0 (IC50 1.1x10-8 M) [36] sunitinib Hs Inhibition 7.9 pIC50 34 ⤷ pIC50 7.9 (IC50 1.31x10-8 M) [34] compound 8i [PMID: 22765894] Hs Inhibition 7.9 pIC50 69 ⤷ pIC50 7.9 (IC50 1.38x10-8 M) [69] linifanib Hs Inhibition 7.8 pIC50 3 ⤷ pIC50 7.8 (IC50 1.4x10-8 M) [3] SU-14813 Hs Inhibition 7.8 pIC50 49 ⤷ pIC50 7.8 (IC50 1.5x10-8 M) [49] edicotinib Hs Inhibition 7.7 pIC50 24 ⤷ pIC50 7.7 (IC50 2x10-8 M) [24] ilorasertib Hs Inhibition 7.7 pIC50 25 ⤷ pIC50 7.7 (IC50 2x10-8 M) [25] Description: Measuring inhibition of kinase activity in a biochemical assay. labuxtinib Hs Inhibition 7.7 pIC50 68 ⤷ pIC50 7.7 (IC50 2x10-8 M) [68] pexidartinib Hs Inhibition >7.6 pIC50 56 ⤷ pIC50 >7.6 (IC50 <2.7x10-8 M) [56] bezuclastinib Hs Inhibition 7.6 pIC50 23 ⤷ pIC50 7.6 (IC50 2.8x10-8 M) [23] Description: Inhibition of KITV560G/D816V AKN-028 Hs Inhibition 7.5 pIC50 14 ⤷ pIC50 7.5 (IC50 2.9x10-8 M) [14] Description: Inhibition of KIT autophosphorylation in human AML M07 cells which overexpress KIT CHMFL-KIT-8140 Hs Inhibition 7.5 pIC50 39 ⤷ pIC50 7.5 (IC50 3.3x10-8 M) [39] M4205 Hs Inhibition 7.4 pIC50 7 ⤷ pIC50 7.4 (IC50 4.4x10-8 M) [7] compound 19a [PMID: 30503936] Hs Inhibition 7.2 pIC50 51 ⤷ pIC50 7.2 (IC50 6.4x10-8 M) [51] sorafenib Hs Inhibition 7.2 pIC50 65,69 ⤷ pIC50 7.2 (IC50 6.8x10-8 M) [69] pIC50 7.2 (IC50 6.8x10-8 M) [65] avapritinib Hs Inhibition 7.1 pIC50 15 ⤷ pIC50 7.1 (IC50 7.3x10-8 M) [15] PLX5622 Hs Inhibition <7.0 pIC50 71 ⤷ pIC50 <7.0 (IC50 >1x10-7 M) [71] Description: Binned IC50 value from patent data OSI-930 Hs Inhibition 6.4 – 7.6 pIC50 22 ⤷ pIC50 6.4 – 7.6 (IC50 4x10-7 – 2.5x10-8 M) [22] Description: The IC50 varied dependent on whether KIT was activated or unactivated, with the lower value measured for the activated enzyme. enrupatinib Hs Inhibition >7.0 pIC50 50 ⤷ pIC50 >7.0 (IC50 <1x10-7 M) [50] Description: Binned value from patent pazopanib Hs Inhibition 6.8 pIC50 29 ⤷ pIC50 6.8 (IC50 1.4x10-7 M) [29] tandutinib Hs Inhibition 6.8 pIC50 33 ⤷ pIC50 6.8 (IC50 1.7x10-7 M) [33] masitinib Hs Inhibition 6.7 pIC50 13 ⤷ pIC50 6.7 (IC50 2x10-7 M) [13] CP-673451 Hs Inhibition 6.6 pIC50 53 ⤷ pIC50 6.6 (IC50 2.52x10-7 M) [53] GTP-14564 Hs Inhibition 6.5 pIC50 44 ⤷ pIC50 6.5 (IC50 3x10-7 M) [44] vimseltinib Hs Inhibition 6.0 – 7.0 pIC50 1 ⤷ pIC50 6.0 – 7.0 (IC50 1x10-6 – 1x10-7 M) [1] semaxanib Hs Inhibition 6.4 pIC50 8 ⤷ pIC50 6.4 (IC50 4x10-7 M) [8] rivoceranib Hs Inhibition 6.4 pIC50 58 ⤷ pIC50 6.4 (IC50 4.29x10-7 M) [58] Description: Assay used apatinib mesylate (YN968D1) Ki-20227 Hs Inhibition 6.3 pIC50 45 ⤷ pIC50 6.3 (IC50 4.51x10-7 M) [45] AST-487 Hs Inhibition 6.3 pIC50 2 ⤷ pIC50 6.3 (IC50 5x10-7 M) [2] Description: In vitro inhibition of c-Kit lucitanib Hs Inhibition 6.3 pIC50 72 ⤷ pIC50 6.3 (IC50 5.27x10-7 M) [72] flumbatinib Hs Inhibition 6.2 pIC50 41 ⤷ pIC50 6.2 (IC50 6.66x10-7 M) [41] sotuletinib Hs Inhibition 5.4 pIC50 55 ⤷ pIC50 5.4 (IC50 3.88x10-6 M) [55] ripretinib Hs Inhibition - - 17 ⤷ [17]
Inhibitor Comments
Note that the primary target of avapritinib (BLU-285) is mutant, constitutively active KIT rather than the wild type kinase [15].

Agonists
Key to terms and symbols		Click column headers to sort
Ligand Sp. Action Value Parameter Reference stem cell factor {Sp: Human} Hs Agonist 9.6 – 9.8 pKd 61 ⤷ pKd 9.6 – 9.8 (Kd 2.4x10-10 – 1.5x10-10 M) [61] Description: Binding affinity of KIT receptors on cell membranes from OCIM1, MO7e and HEL cells, using 125I-SCF as radioligand.

Antibodies
Key to terms and symbols		Click column headers to sort
Antibody Sp. Action Value Parameter Reference barzolvolimab Hs Binding - - 28 ⤷ [28] briquilimab Hs Binding - - 63 ⤷ [63]

DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 12,66
Key to terms and symbols		Click column headers to sort
Target used in screen: KIT
Ligand Sp. Type Action Value Parameter sunitinib Hs Inhibitor Inhibition 9.4 pKd cediranib Hs Inhibitor Inhibition 9.4 pKd SU-14813 Hs Inhibitor Inhibition 9.2 pKd Ki-20227 Hs Inhibitor Inhibition 9.2 pKd dasatinib Hs Inhibitor Inhibition 9.1 pKd PD-173955 Hs Inhibitor Inhibition 8.7 pKd linifanib Hs Inhibitor Inhibition 8.7 pKd foretinib Hs Inhibitor Inhibition 8.6 pKd tandutinib Hs Inhibitor Inhibition 8.6 pKd pazopanib Hs Inhibitor Inhibition 8.6 pKd
Target used in screen: KIT(A829P)
Ligand Sp. Type Action Value Parameter staurosporine Hs Inhibitor Inhibition 9.2 pKd dasatinib Hs Inhibitor Inhibition 9.2 pKd foretinib Hs Inhibitor Inhibition 8.5 pKd tamatinib Hs Inhibitor Inhibition 8.5 pKd quizartinib Hs Inhibitor Inhibition 8.4 pKd AST-487 Hs Inhibitor Inhibition 8.4 pKd masitinib Hs Inhibitor Inhibition 7.9 pKd motesanib Hs Inhibitor Inhibition 7.8 pKd imatinib Hs Inhibitor Inhibition 7.8 pKd linifanib Hs Inhibitor Inhibition 7.8 pKd
Target used in screen: KIT(D816H)
Ligand Sp. Type Action Value Parameter staurosporine Hs Inhibitor Inhibition 9.4 pKd dasatinib Hs Inhibitor Inhibition 8.8 pKd tamatinib Hs Inhibitor Inhibition 8.2 pKd lestaurtinib Hs Inhibitor Inhibition 8.0 pKd midostaurin Hs Inhibitor Inhibition 7.8 pKd foretinib Hs Inhibitor Inhibition 7.4 pKd JNJ-28312141 Hs Inhibitor Inhibition 7.3 pKd AST-487 Hs Inhibitor Inhibition 7.2 pKd sunitinib Hs Inhibitor Inhibition 7.0 pKd tandutinib Hs Inhibitor Inhibition 6.9 pKd
Target used in screen: KIT(D816V)
Ligand Sp. Type Action Value Parameter staurosporine Hs Inhibitor Inhibition 9.2 pKd tamatinib Hs Inhibitor Inhibition 8.6 pKd dasatinib Hs Inhibitor Inhibition 8.6 pKd lestaurtinib Hs Inhibitor Inhibition 8.1 pKd midostaurin Hs Inhibitor Inhibition 8.1 pKd foretinib Hs Inhibitor Inhibition 8.0 pKd JNJ-28312141 Hs Inhibitor Inhibition 7.7 pKd NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd tandutinib Hs Inhibitor Inhibition 7.5 pKd PD-173955 Hs Inhibitor Inhibition 7.5 pKd
Target used in screen: KIT(L576P)
Ligand Sp. Type Action Value Parameter SU-14813 Hs Inhibitor Inhibition 9.5 pKd cediranib Hs Inhibitor Inhibition 9.3 pKd dasatinib Hs Inhibitor Inhibition 9.2 pKd Ki-20227 Hs Inhibitor Inhibition 9.1 pKd sunitinib Hs Inhibitor Inhibition 8.9 pKd motesanib Hs Inhibitor Inhibition 8.9 pKd dovitinib Hs Inhibitor Inhibition 8.8 pKd axitinib Hs Inhibitor Inhibition 8.8 pKd pazopanib Hs Inhibitor Inhibition 8.7 pKd linifanib Hs Inhibitor Inhibition 8.7 pKd
Target used in screen: KIT(V559D)
Ligand Sp. Type Action Value Parameter cediranib Hs Inhibitor Inhibition 9.6 pKd sunitinib Hs Inhibitor Inhibition 9.4 pKd Ki-20227 Hs Inhibitor Inhibition 9.3 pKd axitinib Hs Inhibitor Inhibition 9.3 pKd SU-14813 Hs Inhibitor Inhibition 9.3 pKd dasatinib Hs Inhibitor Inhibition 9.2 pKd PD-173955 Hs Inhibitor Inhibition 8.8 pKd linifanib Hs Inhibitor Inhibition 8.8 pKd foretinib Hs Inhibitor Inhibition 8.7 pKd pazopanib Hs Inhibitor Inhibition 8.6 pKd
Target used in screen: KIT(V559D,T670I)
Ligand Sp. Type Action Value Parameter sunitinib Hs Inhibitor Inhibition 9.6 pKd cediranib Hs Inhibitor Inhibition 9.5 pKd SU-14813 Hs Inhibitor Inhibition 9.3 pKd axitinib Hs Inhibitor Inhibition 8.9 pKd foretinib Hs Inhibitor Inhibition 8.6 pKd linifanib Hs Inhibitor Inhibition 8.4 pKd quizartinib Hs Inhibitor Inhibition 8.2 pKd pazopanib Hs Inhibitor Inhibition 8.2 pKd barasertib-hQPA Hs Inhibitor Inhibition 8.1 pKd staurosporine Hs Inhibitor Inhibition 8.0 pKd
Target used in screen: KIT(V559D,V654A)
Ligand Sp. Type Action Value Parameter sunitinib Hs Inhibitor Inhibition 9.7 pKd SU-14813 Hs Inhibitor Inhibition 9.6 pKd cediranib Hs Inhibitor Inhibition 9.5 pKd dasatinib Hs Inhibitor Inhibition 8.6 pKd dovitinib Hs Inhibitor Inhibition 8.5 pKd Ki-20227 Hs Inhibitor Inhibition 8.5 pKd axitinib