Protein Information

General Information of the Protein

Protein ID	PT00888
Protein Name	Mast/stem cell growth factor receptor Kit
Secondarily Protein Name	Piebald trait protein Proto-oncogene c-Kit Tyrosine-protein kinase Kit p145 c-kit v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Gene Name	KIT
Secondarily Gene Name	SCFR
Sequence	MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Kinase > Protein Kinase > TK protein kinase group > Tyrosine protein kinase PDGFR family
Function	Tyrosine-protein kinase that acts as a cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1, SH2B2/APS and CBL. Activates the AKT1 signaling pathway by phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Activated KIT also transmits signals via GRB2 and activation of RAS, RAF1 and the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3, STAT5A and STAT5B. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. KIT signaling is modulated by protein phosphatases, and by rapid internalization and degradation of the receptor. Activated KIT promotes phosphorylation of the protein phosphatases PTPN6/SHP-1 and PTPRU, and of the transcription factors STAT1, STAT3, STAT5A and STAT5B. Promotes phosphorylation of PIK3R1, CBL, CRK (isoform Crk-II), LYN, MAPK1/ERK2 and/or MAPK3/ERK1, PLCG1, SRC and SHC1. Show/Hide
Uniprot ID	Primary ID: P10721 Secondarily ID: B5A956 D5LXN2 D5M931 F5H8F8 Q6IQ28 Q99662 Q9UM99 Show/Hide
Ensembl ID	ENSG00000157404
HGNC ID	HGNC:6342
Subcellular Location	Cell membrane

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000755 , Ba/F3 c-Kit D816V

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0254853 Compound Info	(NMHE)9-Hydroxy-2,5,11-trimethyl-6H-pyrido[4,3-b]carbazol-2-ium Show/Hide	C18H17N2O+	1
1	IC50 = 10 nM Bioactivity Info	TI LI LO TS
CP0280315 Compound Info	5,11-Dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Show/Hide	C17H14N2O	1
1	IC50 = 10 nM Bioactivity Info	TI LI LO TS
CP0483641 Compound Info	1-(3-Diethylamino-propylamino)-5,11-dimethyl-6H-pyrido[4,3-b]carbazol-9-ol Show/Hide	C24H30N4O	1
1	IC50 < 10 nM Bioactivity Info	TI LI LO TS
CP0559614 Compound Info	2-(2-Diethylamino-ethyl)-9-hydroxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazol-2-ium Show/Hide	C23H28N3O+	1
1	IC50 = 10 nM Bioactivity Info	TI LI LO TS
CP0051733 Compound Info	5,11-dimethyl-2H-pyrido[4,3-b]carbazole Show/Hide	C17H14N2	1
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0541581 Compound Info	9-Bromo-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Show/Hide	C17H13BrN2	1
1	IC50 = 200 nM Bioactivity Info	TI LI LO TS
CP0232374 Compound Info	9-Methoxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazole Show/Hide	C18H16N2O	1
1	IC50 = 300 nM Bioactivity Info	TI LI LO TS
CP0483642 Compound Info	N',N'-diethyl-N-(2-methyl-6,15,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1,3(8),4,6,9,11(16),12,14-octaen-7-yl)propane-1,3-diamine Show/Hide	C22H27N5	1
1	IC50 = 300 nM Bioactivity Info	TI LI LO TS
CP0483638 Compound Info	N',N'-diethyl-N-(9-methoxy-5-methyl-6H-pyrido[4,3-b]carbazol-1-yl)propane-1,3-diamine Show/Hide	C24H30N4O	1
1	IC50 = 600 nM Bioactivity Info	TI LI LO TS
CP0002778 Compound Info	4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide Show/Hide	C29H31N7O	1
1	IC50 = 5000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000077 , Ba/F3

Cell Line Info

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000725 , COLO 320DM

Cell Line Info

Cell Line ID: CL000121 , FDC-P1

Cell Line Info

Cell Line ID: CL000854 , GIST-5R

Cell Line Info

Cell Line ID: CL000122 , GIST-T1

Cell Line Info

Cell Line ID: CL000123 , GIST430

Cell Line Info

Cell Line ID: CL000950 , GIST882

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000138 , M-07e

Cell Line Info

Cell Line ID: CL000532 , NCI-H526

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0002778 Compound Info	4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide Show/Hide	C29H31N7O	23
1	EC50 = 100 nM
2	IC50 = 16.4 nM
3	IC50 = 21.6 nM
4	IC50 = 41 nM
5	IC50 = 52 nM
6	IC50 = 58 nM
7	IC50 = 100 nM
8	IC50 = 370 nM
9	IC50 = 400 nM
10	IC50 = 413 nM
11	IC50 >= 100000 nM
12	Kd = 12.59 nM
13	Kd = 13 nM
14	Kd = 14 nM
15	Kd = 15 nM
16	Kd = 71 nM
17	Kd = 91 nM
18	Kd = 560 nM
19	Kd = 820 nM
20	Kd = 830 nM
21	Kd = 980 nM
22	Kd = 2500 nM
23	Kd = 2900 nM
CP0060454 Compound Info	2-[4-chloro-3-(trifluoromethyl)phenyl]-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]acetamide Show/Hide	C26H20ClF3N2O4	2
1	EC50 < 100 nM
2	IC50 = 4 nM
CP0639448 Compound Info	Imatinib mesilate Show/Hide	C30H35N7O4S	1
1	EC50 = 942.9 nM
CP0690323 Compound Info	N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(6,7-dimethoxy-9H-pyrimido[4,5-b]indol-4-yl)piperazine-1-carbothioamide Show/Hide	C25H26N6O4S	1
1	EC50 = 1198 nM
CP0085333 Compound Info	Amuvatinib Show/Hide	C23H21N5O3S	1
1	EC50 = 31257 nM
CP0135795 Compound Info	1-(5-ethyl-1,2-oxazol-3-yl)-3-[4-[2-[[6-(4-ethylpiperazin-1-yl)pyrimidin-4-yl]amino]-1,3-thiazol-5-yl]phenyl]urea Show/Hide	C25H29N9O2S	13
1	IC50 = 0.02 nM
2	IC50 = 0.12 nM
3	IC50 = 0.18 nM
4	IC50 = 0.67 nM
5	IC50 = 0.81 nM
6	IC50 = 0.89 nM
7	IC50 = 0.98 nM
8	IC50 = 1.37 nM
9	IC50 = 1.66 nM
10	IC50 = 4.14 nM
11	IC50 = 8.56 nM
12	IC50 = 9.27 nM
13	IC50 = 102 nM
CP0002211 Compound Info	N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide Show/Hide	C22H27FN4O2	21
1	IC50 = 0.7 nM
2	IC50 = 1.1 nM
3	IC50 = 2.8 nM
4	IC50 = 8 nM
5	IC50 = 8.9 nM
6	IC50 = 10 nM
7	IC50 = 13.1 nM
8	IC50 = 35 nM
9	IC50 = 264 nM
10	IC50 = 350 nM
11	Kd = 0.21 nM
12	Kd = 0.28 nM
13	Kd = 0.37 nM
14	Kd = 0.41 nM
15	Kd = 0.7 nM
16	Kd = 0.71 nM
17	Kd = 1.3 nM
18	Kd = 43 nM
19	Kd = 110 nM
20	Kd = 380 nM
21	Ki = 4 nM
CP0240254 Compound Info	1-[4-[(6-aminoquinazolin-4-yl)amino]phenyl]-3-[4-chloro-3-(trifluoromethyl)phenyl]urea Show/Hide	C22H16ClF3N6O	2
1	IC50 = 1 nM
2	IC50 = 923 nM
CP0033861 Compound Info	(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril Show/Hide	C21H21FN6O	11
1	IC50 = 1.1 nM
2	IC50 = 3 nM
3	IC50 = 48.3 nM
4	Kd = 1.6 nM
5	Kd = 3.1 nM
6	Kd = 7.2 nM
7	Kd = 7.5 nM
8	Kd = 26 nM
9	Kd = 45 nM
10	Kd = 170 nM
11	Kd = 1400 nM
CP0203090 Compound Info	1-hexyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea Show/Hide	C20H25N5O	1
1	IC50 = 1.4 nM
CP0351448 Compound Info	3-(2-imidazo[1,2-a]pyridin-7-ylethynyl)-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C30H28F3N5O	1
1	IC50 = 1.6 nM
CP0035428 Compound Info	3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide Show/Hide	C29H27F3N6O	3
1	IC50 = 1.7 nM
2	IC50 = 4.9 nM
3	IC50 = 8 nM
CP0203048 Compound Info	1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-(3-phenylpropyl)urea Show/Hide	C23H23N5O	1
1	IC50 = 1.7 nM
CP0205730 Compound Info	1-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]-3-quinolin-3-ylurea Show/Hide	C23H18N6O	1
1	IC50 = 1.9 nM
CP0436766 Compound Info	3-[2-(2-aminopyrimidin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C27H27F3N6O	1
1	IC50 = 1.9 nM
CP0191185 Compound Info	3-[2-(6-aminopyridin-3-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C28H28F3N5O	1
1	IC50 = 2 nM
CP0206230 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(4-tert-butylphenyl)-4-methylpyridin-2(1H)-one Show/Hide	C24H24N4O	1
1	IC50 = 2.1 nM
CP0229003 Compound Info	1-(3-methylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea Show/Hide	C21H19N5O	1
1	IC50 = 2.1 nM
CP0184069 Compound Info	3-[2-(6-amino-5-methylpyridin-3-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C29H30F3N5O	1
1	IC50 = 2.1 nM
CP0270974 Compound Info	4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(pyridin-3-ylethynyl)benzamide Show/Hide	C28H27F3N4O	1
1	IC50 = 2.1 nM
CP0161699 Compound Info	N-[3-fluoro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methyl-3-(2-pyridin-3-ylethynyl)benzamide Show/Hide	C27H27FN4O	1
1	IC50 = 2.3 nM
CP0184289 Compound Info	1-(3-methyl-4-morpholin-4-ylphenyl)-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea Show/Hide	C25H26N6O2	1
1	IC50 = 2.4 nM
CP0368507 Compound Info	1-[4-[3-(hydroxymethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]-3-(3-methylphenyl)urea Show/Hide	C21H19N5O2	1
1	IC50 = 2.4 nM
CP0191187 Compound Info	4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-([1,2,4]triazolo[4,3-a]pyridin-7-yl)ethynyl]benzamide Show/Hide	C29H27F3N6O	1
1	IC50 = 2.5 nM
CP0436767 Compound Info	3-[2-(2-aminopyrimidin-5-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]benzamide Show/Hide	C26H28N6O	1
1	IC50 = 2.6 nM
CP0059308 Compound Info	1-[2-(3-aminophenyl)-5-tert-butylpyrazol-3-yl]-3-[4-(quinazolin-4-ylamino)phenyl]urea Show/Hide	C28H28N8O	2
1	IC50 = 3.3 nM
2	IC50 = 24 nM
CP0303422 Compound Info	3-[2-[2-(2-methoxyethylamino)pyrimidin-5-yl]ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C30H33F3N6O2	1
1	IC50 = 3.3 nM
CP0531605 Compound Info	4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]-3-(2-pyridin-3-ylethynyl)benzamide Show/Hide	C27H28N4O	1
1	IC50 = 3.3 nM
CP0368036 Compound Info	N-[4-[4-[[2-(3-aminophenyl)-5-tert-butylpyrazol-3-yl]carbamoylamino]anilino]quinazolin-6-yl]-3-(4-methylpiperazin-1-yl)propanamide Show/Hide	C36H43N11O2	2
1	IC50 = 3.5 nM
2	IC50 = 6.9 nM
CP0161700 Compound Info	4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-(2-pyridin-2-ylethynyl)benzamide Show/Hide	C28H27F3N4O	1
1	IC50 = 3.5 nM
CP0046394 Compound Info	BMS-907351 Show/Hide	C28H24FN3O5	4
1	IC50 = 4 nM
2	IC50 = 4.6 nM
3	IC50 = 6.6 nM
4	IC50 = 53 nM
CP0184068 Compound Info	3-[2-(1-aminoisoquinolin-4-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C32H30F3N5O	1
1	IC50 = 4 nM
CP0024455 Compound Info	5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C26H32N6O2	1
1	IC50 = 5 nM
CP0298640 Compound Info	(Z)-1-[2-Oxo-3-(1H-pyrrol-2-ylmethylene)-2,3-dihydro-1H-indol-6-yl]-3-phenyl-urea Show/Hide	C20H16N4O2	1
1	IC50 = 5.1 nM
CP0461776 Compound Info	3-[2-(6-aminopyridazin-3-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C27H27F3N6O	1
1	IC50 = 5.8 nM
CP0257073 Compound Info	8-(2,3-dihydro-1H-inden-5-yl)-N-methoxy-2-{[4-(1-methylpiperidin-4-yl)phenyl]amino}-5-oxo-5H,8H-pyrido[2,3-d]pyrimidine-6-carboxamide Show/Hide	C30H32N6O3	1
1	IC50 = 6 nM
CP0180491 Compound Info	1-[2-(3-aminophenyl)-5-tert-butylpyrazol-3-yl]-3-[4-[(6-aminoquinazolin-4-yl)amino]phenyl]urea Show/Hide	C28H29N9O	2
1	IC50 = 6.1 nM
2	IC50 = 7.6 nM
CP0043225 Compound Info	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide Show/Hide	C21H15ClF4N4O3	2
1	IC50 = 6.1 nM
2	IC50 = 7 nM
CP0351447 Compound Info	3-[2-(2-aminopyrimidin-5-yl)ethynyl]-2-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C27H27F3N6O	1
1	IC50 = 6.2 nM
CP0538822 Compound Info	3-[2-(2-aminopyrimidin-5-yl)ethynyl]-N-[3-fluoro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]-4-methylbenzamide Show/Hide	C26H27FN6O	1
1	IC50 = 6.5 nM
CP0448634 Compound Info	3-[2-(3-methoxypyridin-2-yl)ethynyl]-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C29H29F3N4O2	1
1	IC50 = 6.7 nM
CP0448635 Compound Info	3-iodo-4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C21H23F3IN3O	1
1	IC50 = 6.8 nM
CP0096180 Compound Info	1-[5-tert-butyl-2-(3-nitrophenyl)pyrazol-3-yl]-3-[4-(quinazolin-4-ylamino)phenyl]urea Show/Hide	C28H26N8O3	2
1	IC50 = 7.3 nM
2	IC50 = 38 nM
CP0490017 Compound Info	1,4-Hybrid, 5 Show/Hide	C31H33N9O2	2
1	IC50 = 7.6 nM
2	IC50 = 22.1 nM
CP0137971 Compound Info	3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(trifluoromethyl)phenyl)pyridin-2(1H)-one Show/Hide	C21H15F3N4O	1
1	IC50 = 7.9 nM
CP0137970 Compound Info	1-(4-(1H-pyrazol-1-yl)phenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one Show/Hide	C23H18N6O	1
1	IC50 = 10 nM
CP0002230 Compound Info	4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide Show/Hide	C28H22F3N7O	13
1	IC50 < 10 nM
2	IC50 = 14.7 nM
3	IC50 = 158 nM
4	IC50 > 200 nM
5	IC50 > 1000 nM
6	Kd = 17 nM
7	Kd = 22 nM
8	Kd = 29 nM
9	Kd = 46 nM
10	Kd = 150 nM
11	Kd = 260 nM
12	Kd = 540 nM
13	Kd = 770 nM
CP0180471 Compound Info	5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-(2-methylsulfonylethyl)piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C25H31N5O3S	1
1	IC50 = 12 nM
CP0166514 Compound Info	3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-morpholinophenyl)pyridin-2(1H)-one Show/Hide	C24H23N5O2	1
1	IC50 = 13 nM
CP0137972 Compound Info	3-(2-aminoquinazolin-6-yl)-4-methyl-1-(3-(trifluoromethyl)phenyl)pyridin-2(1H)-one Show/Hide	C21H15F3N4O	1
1	IC50 = 14 nM
CP0310155 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(4-fluoro-3-methylphenyl)-4-methylpyridin-2(1H)-one Show/Hide	C21H17FN4O	1
1	IC50 = 14 nM
CP0036099 Compound Info	1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea Show/Hide	C21H18FN5O	10
1	IC50 = 14 nM
2	IC50 = 16 nM
3	Kd = 1.7 nM
4	Kd = 1.9 nM
5	Kd = 2 nM
6	Kd = 3.8 nM
7	Kd = 17 nM
8	Kd = 21 nM
9	Kd = 81 nM
10	Kd = 1100 nM
CP0166510 Compound Info	ethyl 4-[3-(2-aminoquinazolin-6-yl)-4-methyl-2-oxopyridin-1-yl]benzoate Show/Hide	C23H20N4O3	1
1	IC50 = 17 nM
CP0206226 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(4-methoxyphenyl)-4-methylpyridin-2(1H)-one Show/Hide	C21H18N4O2	1
1	IC50 = 17 nM
CP0166511 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(4-chlorophenyl)-4-methylpyridin-2(1H)-one Show/Hide	C20H15ClN4O	1
1	IC50 = 20 nM
CP0206224 Compound Info	1-(4-acetylphenyl)-3-(2-aminoquinazolin-6-yl)-4-methylpyridin-2(1H)-one Show/Hide	C22H18N4O2	1
1	IC50 = 20 nM
CP0137973 Compound Info	3-(2-aminoquinazolin-6-yl)-4-methyl-1-(4-(oxazol-2-yl)phenyl)pyridin-2(1H)-one Show/Hide	C23H17N5O2	1
1	IC50 = 22 nM
CP0179797 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(2-pyrrolidin-1-ylethoxy)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C28H37N5O2	1
1	IC50 = 25 nM
CP0170168 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(3-fluoro-4-methylphenyl)-4-methylpyridin-2(1H)-one Show/Hide	C21H17FN4O	1
1	IC50 = 40 nM
CP0210539 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(2-methoxyethylamino)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C25H33N5O2	1
1	IC50 = 42 nM
CP0222021 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(4-ethylpiperazin-1-yl)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C28H38N6O	1
1	IC50 = 50 nM
CP0103171 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(2-morpholin-4-ylethoxy)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C28H37N5O3	1
1	IC50 = 57 nM
CP0166512 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(4-chloro-3-fluorophenyl)-4-methylpyridin-2(1H)-one Show/Hide	C20H14ClFN4O	1
1	IC50 = 60 nM
CP0206225 Compound Info	3-(2-aminoquinazolin-6-yl)-1-(3-methoxyphenyl)-4-methylpyridin-2(1H)-one Show/Hide	C21H18N4O2	1
1	IC50 = 65 nM
CP0202806 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(2-morpholin-4-ylethylamino)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C28H38N6O2	1
1	IC50 = 92 nM
CP0188938 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[1-(2-methoxyethylamino)-2-methylpropan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C26H35N5O2	1
1	IC50 = 110 nM
CP0538824 Compound Info	4-methyl-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[2-(5-phenylmethoxypyridin-2-yl)ethynyl]benzamide Show/Hide	C35H33F3N4O2	1
1	IC50 = 120.9 nM
CP0226713 Compound Info	1-cyclopentyl-3-[4-(3-methyl-2H-pyrazolo[3,4-b]pyridin-4-yl)phenyl]urea Show/Hide	C19H21N5O	1
1	IC50 = 144 nM
CP0034949 Compound Info	4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]-N-(4-propan-2-yloxyphenyl)piperazine-1-carboxamide Show/Hide	C31H42N6O4	10
1	IC50 = 170 nM
2	IC50 = 220 nM
3	Kd = 2.7 nM
4	Kd = 3.8 nM
5	Kd = 6 nM
6	Kd = 23 nM
7	Kd = 26 nM
8	Kd = 29 nM
9	Kd = 120 nM
10	Kd = 1100 nM
CP0548642 Compound Info	N-[(2R)-2-fluoro-3-hydroxy-3-methylbutyl]-4-(propan-2-ylamino)-6-(pyrazolo[1,5-a]pyrimidin-5-ylamino)pyridine-3-carboxamide Show/Hide	C20H26FN7O2	1
1	IC50 = 170 nM
CP0210538 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-[4-(2-methoxyethyl)piperazin-1-yl]propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C29H40N6O2	1
1	IC50 = 210 nM
CP0006232 Compound Info	4-(6,7-Dimethoxy-quinazolin-4-yl)-piperazine-1-carbothioic acid (benzo[1,3]dioxol-5-ylmethyl)-amide Show/Hide	C23H25N5O4S	1
1	IC50 = 220 nM
CP0202805 Compound Info	5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-4-[2-(1,1-dioxo-1,4-thiazinan-4-yl)propan-2-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C26H33N5O3S	1
1	IC50 = 250 nM
CP0065873 Compound Info	1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2-(dimethylamino)ethanone Show/Hide	C26H29N7O2	1
1	IC50 = 559 nM
CP0661487 Compound Info	3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate Show/Hide	C26H34Cl2N7O7P	1
1	IC50 = 750 nM
CP0351449 Compound Info	2-ethyl-3-iodo-N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide Show/Hide	C22H25F3IN3O	1
1	IC50 = 1039.3 nM
CP0137907 Compound Info	2-(4-methylpiperazin-1-yl)-N-[4-methyl-5-[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]-1,3-thiazol-2-yl]acetamide Show/Hide	C25H27N7OS	1
1	IC50 = 2167 nM
CP0030365 Compound Info	5-amino-N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenylpyrazole-4-carboxamide Show/Hide	C27H33N5O2	1
1	IC50 ~ 8500 nM
CP0080859 Compound Info	N-[2-(dimethylamino)ethyl]-N-[[4-[[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]carbamoyl]phenyl]methyl]pyridine-3-carboxamide Show/Hide	C34H34N8O2	1
1	IC50 > 10000 nM
CP0029924 Compound Info	N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamide Show/Hide	C28H31F3N4O2	1
1	IC50 > 20000 nM
CP0226718 Compound Info	1-(3-methylphenyl)-3-[4-[3-(trifluoromethyl)-2H-pyrazolo[3,4-b]pyridin-4-yl]phenyl]urea Show/Hide	C21H16F3N5O	1
1	IC50 > 50000 nM
CP0010193 Compound Info	AG-013736 Show/Hide	C22H18N4OS	10
1	Kd = 0.49 nM
2	Kd = 1.4 nM
3	Kd = 1.7 nM
4	Kd = 3.2 nM
5	Kd = 3.5 nM
6	Kd = 3.7 nM
7	Kd = 13 nM
8	Kd = 1300 nM
9	Kd = 1800 nM
10	Kd = 4200 nM
CP0113988 Compound Info	CEP-32496 Show/Hide	C24H22F3N5O5	1
1	Kd = 2.4 nM
CP0016677 Compound Info	N-[(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]-N-methylbenzamide Show/Hide	C35H30N4O4	8
1	Kd = 7.7 nM
2	Kd = 16 nM
3	Kd = 41 nM
4	Kd = 43 nM
5	Kd = 150 nM
6	Kd = 200 nM
7	Kd = 220 nM
8	Kd = 1600 nM
CP0037049 Compound Info	CHEMBL1835870 Show/Hide	C23H29N7O	1
1	Ki < 1 nM

Clinical Information about the Protein

Target 1 ( Tyrosine-protein kinase Kit (KIT) )

Target Type	Successful Target
Disease	9 Target-related Diseases				9
1	Chronic myelogenous leukaemia [ICD-11: 2A20.0]
2	Acute lymphoblastic leukaemia [ICD-11: 2A85]
3	Metastatic colorectal cancer [ICD-11: 2B91]
4	Thrombocytopenia [ICD-11: 3B64]
5	Renal cell carcinoma [ICD-11: 2C90]
6	Tenosynovial giant cell tumour [ICD-11: 2F7B]
7	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
8	Gastrointestinal stromal tumour [ICD-11: 2B5B]
9	Non-small-cell lung cancer [ICD-11: 2C25.Y]
Approved Drug(s)	7 Approved Drugs				7
1	Imatinib	Drug Info	Approved	Chronic myelogenous leukaemia
2	Ponatinib	Drug Info	Approved	Acute lymphoblastic leukaemia
3	Regorafenib	Drug Info	Approved	Metastatic colorectal cancer
4	Romiplostim	Drug Info	Approved	Thrombocytopenia
5	Sorafenib	Drug Info	Approved	Renal cell carcinoma
6	Pexidartinib	Drug Info	Approved	Tenosynovial giant cell tumour
7	Ripretinib	Drug Info	Approved	Gastrointestinal stromal tumour
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	Famitinib	Drug Info	Phase 2	Solid tumour/cancer
2	MP470	Drug Info	Phase 2	Solid tumour/cancer
3	OSI-930	Drug Info	Phase 1	Solid tumour/cancer
Discontinued Drug(s)	1 Discontinued Drug				1
1	Motesanib	Drug Info	Discontinued in Phase 3	Non-small-cell lung cancer

Target 2 ( KIT D816V mutant (KIT D816V) )

Target Type	Clinical trial Target
Disease	1 Target-related Disease				1
1	Gastrointestinal stromal tumour [ICD-11: 2B5B]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Bezuclastinib	Drug Info	Phase 3	Gastrointestinal stromal tumour

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han