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KIT proto-oncogene, receptor tyrosine kinase

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1805

Nomenclature: KIT proto-oncogene, receptor tyrosine kinase

Abbreviated Name: Kit

Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 976 4q11-q12 KIT KIT proto-oncogene, receptor tyrosine kinase
Mouse 1 979 5 Kit KIT proto-oncogene receptor tyrosine kinase
Rat - 978 14p11 Kit KIT proto-oncogene receptor tyrosine kinase
Previous and Unofficial Names Click here for help
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 Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the extracellular domain of the receptor tyrosine kinase, Kit
PDB Id:  2EC8
Resolution:  3.0Å
Species:  Human
References:  58
Image of receptor 3D structure from RCSB PDB
Description:  KIT kinase domain in complex with sunitinib
PDB Id:  3G0E
Ligand:  sunitinib
Resolution:  1.6Å
Species:  Human
References:  16
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
stem cell factor {Sp: Human}

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
sunitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.4 pKd 10
pKd 9.4 (Kd 3.7x10-10 M) [10]
AC710 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pKd 33
pKd 9.0 (Kd 1x10-9 M) [33]
quizartinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pKd 8
pKd 8.3 (Kd 4.8x10-9 M) [8]
masitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.1 pKd 10
pKd 8.1 (Kd 8.1x10-9 M) [10]
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pKd 50
pKd 7.6 (Kd 2.6x10-8 M) [50]
crenolanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.1 pKd 26
pKd 7.1 (Kd 7.8x10-8 M) [26]
famitinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 9
pIC50 8.7 (IC50 2x10-9 M) [9]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 – 8.7 pIC50 43,51
pIC50 8.5 – 8.7 (IC50 3x10-9 – 2x10-9 M) [43,51]
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 53
pIC50 8.5 (IC50 3x10-9 M) [53]
CHMFL-KIT-64 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 56
pIC50 8.4 (IC50 4x10-9 M) [56]
Description: In a biochemical assay.
CS2164 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 60
pIC50 8.4 (IC50 4x10-9 M) [60]
Description: Inhibition in a biochemical assay.
compound 7k [PMID: 23521020] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 18
pIC50 8.3 (IC50 4.89x10-9 M) [18]
JNJ-28312141 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pIC50 35
pIC50 8.3 (IC50 5x10-9 M) [35]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 40
pIC50 8.2 (IC50 6x10-9 M) [40]
Description: In a biochemical enzyme activity assay.
henatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 9
pIC50 8.1 (IC50 8x10-9 M) [9]
SU11652 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 14
pIC50 8.0 (IC50 1x10-8 M) [14]
KBP-7018 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 8.0 pIC50 27
pIC50 8.0 (IC50 1x10-8 M) [27]
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 31
pIC50 8.0 (IC50 1.1x10-8 M) [31]
sunitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 30
pIC50 7.9 (IC50 1.31x10-8 M) [30]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.9 pIC50 57
pIC50 7.9 (IC50 1.38x10-8 M) [57]
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.4x10-8 M) [3]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.8 pIC50 41
pIC50 7.8 (IC50 1.5x10-8 M) [41]
edicotinib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.7 pIC50 21
pIC50 7.7 (IC50 2x10-8 M) [21]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 22
pIC50 7.7 (IC50 2x10-8 M) [22]
Description: Measuring inhibition of kinase activity in a biochemical assay.
pexidartinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition >7.6 pIC50 47
pIC50 >7.6 (IC50 <2.7x10-8 M) [47]
AKN-028 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 12
pIC50 7.5 (IC50 2.9x10-8 M) [12]
Description: Inhibition of KIT autophosphorylation in human AML M07 cells which overexpress KIT
CHMFL-KIT-8140 Small molecule or natural product Hs Inhibition 7.5 pIC50 32
pIC50 7.5 (IC50 3.3x10-8 M) [32]
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.2 pIC50 42
pIC50 7.2 (IC50 6.4x10-8 M) [42]
sorafenib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pIC50 54,57
pIC50 7.2 (IC50 6.8x10-8 M) [57]
pIC50 7.2 (IC50 6.8x10-8 M) [54]
avapritinib Small molecule or natural product Approved drug Immunopharmacology Ligand Hs Inhibition 7.1 pIC50 13
pIC50 7.1 (IC50 7.3x10-8 M) [13]
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 – 7.6 pIC50 20
pIC50 6.4 – 7.6 (IC50 4x10-7 – 2.5x10-8 M) [20]
Description: The IC50 varied dependent on whether KIT was activated or unactivated, with the lower value measured for the activated enzyme.
pazopanib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.8 pIC50 25
pIC50 6.8 (IC50 1.4x10-7 M) [25]
tandutinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 29
pIC50 6.8 (IC50 1.7x10-7 M) [29]
masitinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 11
pIC50 6.7 (IC50 2x10-7 M) [11]
CP-673451 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 44
pIC50 6.6 (IC50 2.52x10-7 M) [44]
GTP-14564 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.5 pIC50 37
pIC50 6.5 (IC50 3x10-7 M) [37]
DCC-3014 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 – 7.0 pIC50 1
pIC50 6.0 – 7.0 (IC50 1x10-6 – 1x10-7 M) [1]
semaxanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pIC50 7
pIC50 6.4 (IC50 4x10-7 M) [7]
rivoceranib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.4 pIC50 49
pIC50 6.4 (IC50 4.29x10-7 M) [49]
Description: Assay used apatinib mesylate (YN968D1)
Ki-20227 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 38
pIC50 6.3 (IC50 4.51x10-7 M) [38]
AST-487 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 2
pIC50 6.3 (IC50 5x10-7 M) [2]
Description: In vitro inhibition of c-Kit
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 59
pIC50 6.3 (IC50 5.27x10-7 M) [59]
flumatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.2 pIC50 34
pIC50 6.2 (IC50 6.66x10-7 M) [34]
BLZ945 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.4 pIC50 46
pIC50 5.4 (IC50 3.88x10-6 M) [46]
ripretinib Small molecule or natural product Approved drug Hs Inhibition - - 15
[15]
Inhibitor Comments
Note that the primary target of avapritinib (BLU-285) is mutant, constitutively active KIT rather than the wild type kinase [13].
Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
stem cell factor {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Agonist 9.6 – 9.8 pKd 52
pKd 9.6 – 9.8 (Kd 2.4x10-10 – 1.5x10-10 M) [52]
Description: Binding affinity of KIT receptors on cell membranes from OCIM1, MO7e and HEL cells, using 125I-SCF as radioligand.
DiscoveRx KINOMEscan® screen Click here for help
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: 10,55

Key to terms and symbols Click column headers to sort
Target used in screen: KIT
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.4 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.4 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.2 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.2 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.1 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
tandutinib Small molecule or natural product Hs Inhibitor Inhibition 8.6 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 8.6 pKd
Target used in screen: KIT(A829P)
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.5 pKd
quizartinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 7.8 pKd
Target used in screen: KIT(D816H)
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.8 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
tandutinib Small molecule or natural product Hs Inhibitor Inhibition 6.9 pKd
Target used in screen: KIT(D816V)
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
tandutinib Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
Target used in screen: KIT(L576P)
Ligand Sp. Type Action Value Parameter
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 8.8 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 8.7 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.7 pKd
Target used in screen: KIT(V559D)
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.4 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.8 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 8.6 pKd
Target used in screen: KIT(V559D,T670I)
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.6 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.3 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.4 pKd
quizartinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 8.2 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
Target used in screen: KIT(V559D,V654A)
Ligand Sp. Type Action Value Parameter
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.7 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 9.6 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.5 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 8.5 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
masitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
JNJ-28312141 Small molecule or natural product Hs Inhibitor Inhibition 8.2 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
Target used in screen: KIT-autoinhibited
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.9 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 7.3 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
quizartinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 5.9 pKd
vatalanib Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
sorafenib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.7 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 5.3 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 4,19

Key to terms and symbols Click column headers to sort
Target used in screen: cKit/c-Kit
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.3
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.7
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 9.5 1.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 9.9
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 10.9
Flt-3 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 20.3 1.0 1.0
dorsomorphin Small molecule or natural product