Protein Information

General Information of the Protein

Protein ID	PT01204
Protein Name	Receptor-type tyrosine-protein kinase FLT3
Secondarily Protein Name	FL cytokine receptor Fetal liver kinase-2 Fms-like tyrosine kinase 3 Stem cell tyrosine kinase 1
Gene Name	FLT3
Secondarily Gene Name	CD135 FLK2 STK1
Sequence	MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS 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 FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation of FES, FER, PTPN6/SHP, PTPN11/SHP-2, PLCG1, and STAT5A and/or STAT5B. Activation of wild-type FLT3 causes only marginal activation of STAT5A or STAT5B. Mutations that cause constitutive kinase activity promote cell proliferation and resistance to apoptosis via the activation of multiple signaling pathways. Show/Hide
Uniprot ID	Primary ID: P36888 Secondarily ID: A0AVG9 B7ZLT7 B7ZLT8 F5H0A0 Q13414 Show/Hide
HGNC ID	HGNC:3765
Subcellular Location	Membrane Endoplasmic reticulum lumen

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: CL000605 , 32D

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0641297 Compound Info	N-(5-ethyl-3-isoxazolyl)-N'-[4-(2-[6-(4-ethylpiperazino)-2-methyl-4-pyrimidinyl]amino-1,3-thiazol-5-yl)phenyl]urea Show/Hide	C26H31N9O2S	4
1	GI50 = 4 nM Bioactivity Info	TI LI LO TS
2	GI50 = 6 nM Bioactivity Info	TI LI LO TS
3	GI50 = 38 nM Bioactivity Info	TI LI LO TS
4	GI50 = 70 nM Bioactivity Info	TI LI LO TS
CP0030740 Compound Info	1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea Show/Hide	C29H32N6O4S	4
1	GI50 = 16 nM Bioactivity Info	TI LI LO TS
2	GI50 = 27 nM Bioactivity Info	TI LI LO TS
3	GI50 = 150 nM Bioactivity Info	TI LI LO TS
4	GI50 = 220 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000768 , AML-1

Cell Line Info

Cell Line ID: CL000077 , Ba/F3

Cell Line Info

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000075 , EoL-1

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000071 , MOLM-13

Cell Line Info

Cell Line ID: CL000408 , MOLM-14

Cell Line Info

Cell Line ID: CL000091 , MV4-11

Cell Line Info

Cell Line ID: CL000120 , RS4;11

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
CP0019908 Compound Info	BDBM50242742 Show/Hide	C30H40ClN7O3S	12
1	EC50 = 500 nM
2	IC50 = 3 nM
3	IC50 = 120 nM
4	IC50 = 218 nM
5	IC50 = 536 nM
6	Kd = 2 nM
7	Kd = 4.9 nM
8	Kd = 8.2 nM
9	Kd = 8.6 nM
10	Kd = 11 nM
11	Kd = 15 nM
12	Kd = 34 nM
CP0092370 Compound Info	1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine Show/Hide	C26H29N5O2	6
1	IC50 = 0.06 nM
2	IC50 = 0.3 nM
3	IC50 = 1.3 nM
4	IC50 = 3 nM
5	IC50 = 4 nM
6	IC50 = 35 nM
CP0031589 Compound Info	Gilteritinib Show/Hide	C29H44N8O3	4
1	IC50 = 0.29 nM
2	IC50 = 11000 nM
3	Ki = 2 nM
4	Ki = 10 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 = 0.3 nM
2	IC50 = 12.6 nM
3	IC50 = 13 nM
CP0030740 Compound Info	1-(5-Tert-Butyl-1,2-Oxazol-3-Yl)-3-(4-{7-[2-(Morpholin-4-Yl)ethoxy]imidazo[2,1-B][1,3]benzothiazol-2-Yl}phenyl)urea Show/Hide	C29H32N6O4S	28
1	IC50 < 0.51 nM
2	IC50 = 0.9 nM
3	IC50 = 2 nM
4	IC50 = 2.6 nM
5	IC50 = 4.1 nM
6	IC50 = 4.2 nM
7	IC50 = 4.8 nM
8	IC50 = 6.51 nM
9	IC50 = 7.4 nM
10	IC50 = 10 nM
11	IC50 = 12 nM
12	IC50 = 30 nM
13	IC50 = 39 nM
14	IC50 = 69 nM
15	IC50 = 93 nM
16	IC50 = 120 nM
17	IC50 = 137 nM
18	IC50 = 170 nM
19	IC50 = 258.2 nM
20	IC50 = 1330 nM
21	Kd = 1.3 nM
22	Kd = 1.6 nM
23	Kd = 2.2 nM
24	Kd = 3.7 nM
25	Kd = 4.1 nM
26	Kd = 5.1 nM
27	Kd = 7.1 nM
28	Kd = 8.8 nM
CP0046394 Compound Info	BMS-907351 Show/Hide	C28H24FN3O5	5
1	IC50 = 0.6 nM
2	IC50 = 6 nM
3	IC50 = 11.3 nM
4	IC50 = 25 nM
5	IC50 = 418 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	25
1	IC50 = 0.7 nM
2	IC50 = 0.8 nM
3	IC50 = 1.4 nM
4	IC50 = 2.5 nM
5	IC50 = 3 nM
6	IC50 = 4.7 nM
7	IC50 = 5 nM
8	IC50 = 6.5 nM
9	IC50 = 8 nM
10	IC50 = 12 nM
11	IC50 = 21 nM
12	IC50 = 25 nM
13	IC50 = 30 nM
14	IC50 = 50 nM
15	IC50 = 250 nM
16	IC50 = 550 nM
17	Kd = 0.22 nM
18	Kd = 0.41 nM
19	Kd = 0.47 nM
20	Kd = 0.8 nM
21	Kd = 0.99 nM
22	Kd = 2.3 nM
23	Kd = 2.4 nM
24	Kd = 4.3 nM
25	Kd = 11 nM
CP0051296 Compound Info	CHEMBL3326006 Show/Hide	C28H40N6O	1
1	IC50 = 0.8 nM
CP0362727 Compound Info	N-[5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-4-methyl-1H-pyrrol-3-yl]-3-pyrrolidin-1-ylpropanamide Show/Hide	C21H23FN4O2	3
1	IC50 = 0.8 nM
2	IC50 = 1.8 nM
3	IC50 = 1.9 nM
CP0025156 Compound Info	US8623885, 5 Show/Hide	C26H29N7O2	4
1	IC50 = 1 nM
2	IC50 = 1.5 nM
3	Kd = 1 nM
4	Kd = 4 nM
CP0018477 Compound Info	4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide Show/Hide	C21H16ClF3N4O3	18
1	IC50 = 1.3 nM
2	IC50 = 2.8 nM
3	IC50 = 4 nM
4	IC50 = 15.48 nM
5	IC50 = 32.6 nM
6	IC50 = 33 nM
7	IC50 = 54 nM
8	IC50 = 58 nM
9	IC50 = 62 nM
10	IC50 = 103.5 nM
11	Kd = 4.5 nM
12	Kd = 11 nM
13	Kd = 13 nM
14	Kd = 17 nM
15	Kd = 20 nM
16	Kd = 30 nM
17	Kd = 79 nM
18	Kd = 82 nM
CP0645833 Compound Info	(3S,8S,9S)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10,11,12-hexahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione Show/Hide	C19H24O7	5
1	IC50 = 1.59 nM
2	IC50 = 1.8 nM
3	IC50 = 11 nM
4	IC50 = 36 nM
5	IC50 = 62 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 = 2.3 nM
CP0033861 Compound Info	(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril Show/Hide	C21H21FN6O	8
1	IC50 = 3 nM
2	Kd = 0.64 nM
3	Kd = 1.1 nM
4	Kd = 3.6 nM
5	Kd = 4.8 nM
6	Kd = 5.2 nM
7	Kd = 6.1 nM
8	Kd = 7.5 nM
CP0034962 Compound Info	16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one Show/Hide	C26H21N3O4	10
1	IC50 = 3 nM
2	IC50 = 5 nM
3	IC50 = 8.2 nM
4	Kd = 0.57 nM
5	Kd = 0.66 nM
6	Kd = 1.4 nM
7	Kd = 1.5 nM
8	Kd = 5.4 nM
9	Kd = 7 nM
10	Kd = 8.5 nM
CP0024670 Compound Info	CHEMBL3237710 Show/Hide	C27H35N9	1
1	IC50 = 4 nM
CP0065750 Compound Info	1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)phenyl]urea Show/Hide	C19H12ClF3N6O2	3
1	IC50 = 4 nM
2	IC50 = 39 nM
3	Kd = 4.3 nM
CP0121981 Compound Info	3-[1-[3-(dimethylamino)propyl]pyrazol-4-yl]-7-(1H-pyrazol-4-yl)-5H-indeno[1,2-b]indol-10-one Show/Hide	C26H24N6O	2
1	IC50 = 4 nM
2	IC50 = 10 nM
CP0007710 Compound Info	2-[[1-[2-fluoro-4-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]phenyl]piperidin-4-yl]-methylamino]ethanol Show/Hide	C25H34FN7O	1
1	IC50 = 4 nM
CP0139586 Compound Info	(10S,12Z,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione Show/Hide	C22H22O7	1
1	IC50 = 4.37 nM
CP0036099 Compound Info	1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea Show/Hide	C21H18FN5O	11
1	IC50 = 5 nM
2	IC50 = 7 nM
3	IC50 = 12 nM
4	IC50 = 20 nM
5	Kd = 0.63 nM
6	Kd = 1.3 nM
7	Kd = 2.6 nM
8	Kd = 2.7 nM
9	Kd = 8.8 nM
10	Kd = 11 nM
11	Kd = 16 nM
CP0133124 Compound Info	5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine Show/Hide	C20H15ClF3N5	4
1	IC50 = 5 nM
2	IC50 = 7.1 nM
3	IC50 = 11 nM
4	IC50 = 130 nM
CP0041633 Compound Info	[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone Show/Hide	C20H20N4O	7
1	IC50 = 6.6 nM
2	IC50 = 13.1 nM
3	Kd = 6.6 nM
4	Kd = 13 nM
5	Kd = 15 nM
6	Kd = 20 nM
7	Kd = 60 nM
CP0164979 Compound Info	1-[4-(4-amino-7-prop-2-enylpyrrolo[2,3-d]pyrimidin-5-yl)phenyl]-3-(5-tert-butyl-1,2-oxazol-3-yl)urea Show/Hide	C23H25N7O2	1
1	IC50 = 7 nM
CP0146994 Compound Info	1-[4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)phenyl]-3-[3-(trifluoromethyl)phenyl]urea Show/Hide	C19H13F3N6O2	2
1	IC50 = 9 nM
2	Kd = 6.6 nM
CP0278627 Compound Info	benzyl N-[[4-[3-[[4-(2-pyrrolidin-1-ylethoxy)benzoyl]amino]-1H-pyrazol-5-yl]phenyl]methyl]carbamate Show/Hide	C31H33N5O4	1
1	IC50 = 10 nM
CP0073265 Compound Info	3-(4-fluorophenyl)-7-thiophen-2-ylimidazo[1,2-a]pyridine Show/Hide	C17H11FN2S	1
1	IC50 = 15 nM
CP0183209 Compound Info	3-(4-fluorophenyl)-7-phenylimidazo[1,2-a]pyridine Show/Hide	C19H13FN2	1
1	IC50 = 16 nM
CP0357574 Compound Info	(E)-1-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-4-phenylbut-2-ene-1,4-dione Show/Hide	C30H30N6O2	1
1	IC50 = 16 nM
CP0069769 Compound Info	N-[2-chloro-4-(2-morpholin-4-ylethoxy)phenyl]-7-(1H-1,2,4-triazol-5-yl)benzo[c][2,6]naphthyridin-5-amine Show/Hide	C26H24ClN7O2	1
1	IC50 = 17 nM
CP0249330 Compound Info	(10S,12Z)-6-hydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(20),2(7),3,5,12,17(21),18-heptaene-8,14-dione Show/Hide	C22H22O5	1
1	IC50 = 17 nM
CP0561585 Compound Info	(E)-1-(4-methylphenyl)-4-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-ene-1,4-dione Show/Hide	C31H32N6O2	1
1	IC50 = 18 nM
CP0026231 Compound Info	ONX-0803 Show/Hide	C28H32N4O3	2
1	IC50 = 22 nM
2	IC50 = 23 nM
CP0036253 Compound Info	5-(2-chloroanilino)-N-methylbenzo[c][2,6]naphthyridine-7-carboxamide Show/Hide	C20H15ClN4O	1
1	IC50 = 23 nM
CP0102970 Compound Info	5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-(2-morpholin-4-ylethyl)piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide Show/Hide	C28H36N6O2	1
1	IC50 = 23 nM
CP0143654 Compound Info	(E)-4-(dimethylamino)-1-[7-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-en-1-one Show/Hide	C26H33N7O	1
1	IC50 = 23 nM
CP0219569 Compound Info	methyl (E)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-enoate Show/Hide	C25H30N6O2	1
1	IC50 = 23 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 = 30 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	IC50 = 30 nM
2	IC50 = 501 nM
3	Kd = 2 nM
4	Kd = 6 nM
5	Kd = 6.8 nM
6	Kd = 11 nM
7	Kd = 12 nM
8	Kd = 15 nM
CP0136525 Compound Info	(E)-1-(4-methylphenyl)-4-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-ene-1,4-dione Show/Hide	C31H32N6O2	1
1	IC50 = 30 nM
CP0273579 Compound Info	N-[(3,4-dimethoxyphenyl)methyl]-1-phenylbenzimidazol-5-amine Show/Hide	C22H21N3O2	2
1	IC50 = 30 nM
2	IC50 = 90 nM
CP0146995 Compound Info	1-[4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)phenyl]-3-[4-(trifluoromethyl)phenyl]urea Show/Hide	C19H13F3N6O2	2
1	IC50 = 32 nM
2	Kd = 910 nM
CP0016203 Compound Info	Bis-(5-hydroxy-1H-indol-2-yl)-methanone Show/Hide	C17H12N2O3	1
1	IC50 = 33 nM
CP0357998 Compound Info	(E)-1-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-4-phenylbut-2-ene-1,4-dione Show/Hide	C30H30N6O2	1
1	IC50 = 34 nM
CP0152361 Compound Info	3-chloro-4-[[7-(1H-1,2,4-triazol-5-yl)benzo[c][2,6]naphthyridin-5-yl]amino]phenol Show/Hide	C20H13ClN6O	1
1	IC50 = 39 nM
CP0115610 Compound Info	CHEMBL4283353 Show/Hide	C30H44N6O	2
1	IC50 = 39 nM
2	Ki = 16.14 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 = 40 nM
CP0273351 Compound Info	3-(4-fluorophenyl)-7-(furan-2-yl)imidazo[1,2-a]pyridine Show/Hide	C17H11FN2O	1
1	IC50 = 41 nM
CP0558016 Compound Info	(10S,12Z,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione Show/Hide	C22H22O7	1
1	IC50 = 41 nM
CP0001250 Compound Info	(16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene Show/Hide	C23H24N4O	2
1	IC50 = 42 nM
2	IC50 = 56 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 = 58 nM
CP0013877 Compound Info	CERITINIB Show/Hide	C28H36ClN5O3S	1
1	IC50 = 60 nM
CP0210320 Compound Info	N-[2-fluoro-4-(2-pyrrolidin-1-ylethoxy)phenyl]-7-(1H-1,2,4-triazol-5-yl)benzo[c][2,6]naphthyridin-5-amine Show/Hide	C26H24FN7O	1
1	IC50 = 61 nM
CP0466385 Compound Info	(E)-4-(dimethylamino)-1-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]but-2-en-1-one Show/Hide	C26H33N7O	1
1	IC50 = 62 nM
CP0029241 Compound Info	(5-Hydroxy-1H-indol-2-yl)-(4-methyl-1H-indol-2-yl)-methanone Show/Hide	C18H14N2O2	1
1	IC50 = 70 nM
CP0083301 Compound Info	N-(2-fluorophenyl)-7-(1H-1,2,4-triazol-5-yl)benzo[c][2,6]naphthyridin-5-amine Show/Hide	C20H13FN6	1
1	IC50 = 70 nM
CP0007430 Compound Info	IBRUTINIB Show/Hide	C25H24N6O2	2
1	IC50 = 73 nM
2	IC50 > 1000 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	16
1	IC50 = 86.5 nM
2	IC50 = 102 nM
3	IC50 = 200 nM
4	IC50 = 220 nM
5	IC50 = 270 nM
6	IC50 = 290 nM
7	IC50 = 2444 nM
8	IC50 = 9220 nM
9	Kd = 1.5 nM
10	Kd = 3 nM
11	Kd = 3.5 nM
12	Kd = 9.1 nM
13	Kd = 29 nM
14	Kd = 310 nM
15	Kd = 410 nM
16	Kd = 1800 nM
CP0329747 Compound Info	(2,6-dimethylpyridin-4- yl)(4-(7-((1R,4S)-4- hydroxycyclohexyl)-2- (((S)-pentan-2-yl)amino)- 7H-pyrrolo[2,3- d]pyrimidin-5-yl)piperidin- 1-yl)methanone Show/Hide	C30H42N6O2	2
1	IC50 = 90 nM
2	Ki = 41.9 nM
CP0255934 Compound Info	5-fluoro-3-[[4-[2-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]ethoxy]-3-methylazulen-1-yl]methylidene]-1H-indol-2-one Show/Hide	C27H27FN2O3	1
1	IC50 = 98 nM
CP0016361 Compound Info	N-(2-chlorophenyl)-7-(1H-1,2,4-triazol-5-yl)benzo[c][2,6]naphthyridin-5-amine Show/Hide	C20H13ClN6	1
1	IC50 = 104 nM
CP0142408 Compound Info	2-[6-[[5-methyl-4-(1-propan-2-ylpyrazol-4-yl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]acetonitrile Show/Hide	C22H25N7	1
1	IC50 = 108 nM
CP0139006 Compound Info	(10S,12Z,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione Show/Hide	C22H22O7	1
1	IC50 = 110 nM
CP0093136 Compound Info	1-[[6-(hydroxymethyl)-5-methyl-2-thiophen-2-ylthieno[2,3-d]pyrimidin-4-yl]amino]-3-methylpyrrole-2,5-dione Show/Hide	C17H14N4O3S2	2
1	IC50 = 112 nM
2	IC50 = 175 nM
CP0012237 Compound Info	1-[4-[(1R)-1-[2-[[6-[6-(dimethylamino)pyrimidin-4-yl]-1H-benzimidazol-2-yl]amino]pyridin-4-yl]ethyl]piperazin-1-yl]-3,3,3-trifluoropropan-1-one Show/Hide	C27H30F3N9O	2
1	IC50 = 123 nM
2	IC50 > 20000 nM
CP0196758 Compound Info	(3E)-5-chloro-3-[[5-[3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl]furan-2-yl]methylidene]-1H-indol-2-one Show/Hide	C26H24ClN3O3	1
1	IC50 = 134 nM
CP0026540 Compound Info	(4-Methyl-1H-indol-2-yl)-[5-(2-piperidin-1-yl-ethoxy)-1H-indol-2-yl]-methanone Show/Hide	C25H27N3O2	1
1	IC50 = 220 nM
CP0263163 Compound Info	2-amino-1-ethyl-7-[(3R)-3-hydroxy-4-methoxy-3-methylbut-1-ynyl]-N-methyl-4-oxo-1,8-naphthyridine-3-carboxamide Show/Hide	C18H22N4O4	1
1	IC50 = 290 nM
CP0139002 Compound Info	(10S,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione Show/Hide	C22H24O7	1
1	IC50 = 370 nM
CP0047745 Compound Info	N-[5-[4-(benzenesulfonamido)phenyl]-1H-pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide Show/Hide	C27H28N6O3S	1
1	IC50 = 590 nM
CP0000866 Compound Info	6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one Hydrochloride Show/Hide	C24H29N7O2	2
1	IC50 = 3480 nM
2	IC50 > 10000 nM
CP0165545 Compound Info	(10S,12Z,15R,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-14-methylidene-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one Show/Hide	C23H24O6	1
1	IC50 = 4530 nM
CP0356481 Compound Info	(10S,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione Show/Hide	C22H24O7	1
1	IC50 = 7393 nM
CP0531968 Compound Info	(10S,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione Show/Hide	C22H24O7	1
1	IC50 = 7800 nM
CP0245111 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-5-[2-methyl-4-(1,3,5-trimethylpyrazol-4-yl)phenyl]-1,3,4-oxadiazol-2-amine Show/Hide	C24H25N7O	1
1	IC50 = 15848.93 nM
CP0545741 Compound Info	4-[4-[5-[imidazo[1,2-a]pyridin-6-ylmethyl(methyl)amino]-1,3,4-oxadiazol-2-yl]-3-methylphenyl]-2,5-dimethylpyrazole-3-carbonitrile Show/Hide	C24H22N8O	1
1	IC50 = 15848.93 nM
CP0494149 Compound Info	5-[2-chloro-4-(1,3,5-trimethylpyrazol-4-yl)phenyl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C23H22ClN7O	1
1	IC50 = 19952.62 nM
CP0554525 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-5-[3-methyl-5-(1,3,5-trimethylpyrazol-4-yl)pyridin-2-yl]-1,3,4-oxadiazol-2-amine Show/Hide	C23H24N8O	1
1	IC50 = 19952.62 nM
CP0032282 Compound Info	(6-Chloro-1H-indol-2-yl)-(5-methoxy-1H-indol-2-yl)-methanone Show/Hide	C18H13ClN2O2	1
1	IC50 = 23930 nM
CP0487262 Compound Info	4-[4-[5-[imidazo[1,2-a]pyridin-6-ylmethyl(methyl)amino]-1,3,4-oxadiazol-2-yl]-3-methylphenyl]-1,5-dimethylpyrazole-3-carbonitrile Show/Hide	C24H22N8O	1
1	IC50 = 25118.86 nM
CP0257794 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-5-[2-methoxy-4-(1,3,5-trimethylpyrazol-4-yl)phenyl]-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C24H25N7O2	1
1	IC50 = 39810.72 nM
CP0271463 Compound Info	5-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-2-methylphenyl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C23H23N7O	1
1	IC50 = 39810.72 nM
CP0480275 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-5-[2-methyl-4-(2,3,5-trimethylimidazol-4-yl)phenyl]-1,3,4-oxadiazol-2-amine Show/Hide	C24H25N7O	1
1	IC50 = 39810.72 nM
CP0354548 Compound Info	5-[4-(1,5-dimethylpyrazol-4-yl)-2-methylphenyl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C23H23N7O	1
1	IC50 = 63095.73 nM
CP0540377 Compound Info	2-[5-[imidazo[1,2-a]pyridin-6-ylmethyl(methyl)amino]-1,3,4-oxadiazol-2-yl]-5-(1,3,5-trimethylpyrazol-4-yl)benzonitrile Show/Hide	C24H22N8O	1
1	IC50 = 79432.82 nM
CP0245112 Compound Info	5-[4-[1-(difluoromethyl)-3,5-dimethylpyrazol-4-yl]-2-methylphenyl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C24H23F2N7O	1
1	IC50 = 100000 nM
CP0553528 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-5-[4-(1,3,5-trimethylpyrazol-4-yl)phenyl]-1,3,4-oxadiazol-2-amine Show/Hide	C23H23N7O	1
1	IC50 > 63095.73 nM
CP0343136 Compound Info	5-[2-fluoro-4-(1,3,5-trimethylpyrazol-4-yl)phenyl]-N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-1,3,4-oxadiazol-2-amine Show/Hide	C23H22FN7O	1
1	IC50 > 100000 nM
CP0368045 Compound Info	N-(imidazo[1,2-a]pyridin-6-ylmethyl)-N-methyl-5-[2-methyl-6-(1,3,5-trimethylpyrazol-4-yl)pyridin-3-yl]-1,3,4-oxadiazol-2-amine Show/Hide	C23H24N8O	1
1	IC50 > 100000 nM
CP0041572 Compound Info	BDBM50249542 Show/Hide	C22H23FN6O5	7
1	Kd = 0.37 nM
2	Kd = 0.54 nM
3	Kd = 0.65 nM
4	Kd = 0.68 nM
5	Kd = 0.71 nM
6	Kd = 1.5 nM
7	Kd = 4.4 nM
CP0127888 Compound Info	AB-460 Show/Hide	C24H23N5O3	1
1	Kd = 1.1 nM
CP0061797 Compound Info	Benzo[d]imidazo[2,1-b]thiazole-2-carboxylic acid {4-[3-(5-tert-butyl-isoxazol-3-yl)-ureido]-phenyl}-amide Show/Hide	C24H22N6O3S	1
1	Kd = 1.6 nM
CP0034613 Compound Info	N-[(2S,3R,4R,6R,18S)-18-hydroxy-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	C35H30N4O5	1
1	Kd = 68 nM
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	2
1	Kd = 6300 nM
2	Kd > 10000 nM
CP0037049 Compound Info	CHEMBL1835870 Show/Hide	C23H29N7O	2
1	Ki = 0.17 nM
2	Ki = 2 nM

Clinical Information about the Protein

Target 1 ( Fms-like tyrosine kinase 3 (FLT-3) )

Target Type	Successful Target
Disease	11 Target-related Diseases				11
1	Acute myeloid leukaemia [ICD-11: 2A60]
2	Acute lymphoblastic leukaemia [ICD-11: 2A85]
3	Human immunodeficiency virus infection [ICD-11: 1C62]
4	Myelofibrosis [ICD-11: 2A20.2]
5	Tenosynovial giant cell tumour [ICD-11: 2F7B]
6	Chronic pain [ICD-11: MG30]
7	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
8	Alzheimer disease [ICD-11: 8A20]
9	Diffuse large B-cell lymphoma [ICD-11: 2A81]
10	Anaplastic mixed oligoastrocytoma [ICD-11: 2A00.0Y]
11	Airway inflammation [ICD-11: CA05]
Approved Drug(s)	8 Approved Drugs				8
1	Gilteritinib	Drug Info	Approved	Acute myeloid leukaemia
2	Lestaurtinib	Drug Info	Approved (orphan drug)	Acute myeloid leukaemia
3	Midostaurin	Drug Info	Approved	Acute myeloid leukaemia
4	Ponatinib	Drug Info	Approved	Acute lymphoblastic leukaemia
5	Zidovudine	Drug Info	Approved	Human immunodeficiency virus infection
6	Pacritinib	Drug Info	Approved	Myelofibrosis
7	Pexidartinib	Drug Info	Approved	Tenosynovial giant cell tumour
8	Quizartinib	Drug Info	Approved	Acute myeloid leukaemia
Clinical Trial Drug(s)	7 Clinical Trial Drugs				7
1	BMS-690514	Drug Info	Phase 2	Chronic pain
2	Famitinib	Drug Info	Phase 2	Solid tumour/cancer
3	FF-10101	Drug Info	Phase 1/2	Acute myeloid leukaemia
4	MK-2461	Drug Info	Phase 1/2	Alzheimer disease
5	TAK-659	Drug Info	Phase 2	Diffuse large B-cell lymphoma
6	FN-1501	Drug Info	Phase 1	Solid tumour/cancer
7	KW-2449	Drug Info	Phase 1	Acute myeloid leukaemia
Discontinued Drug(s)	2 Discontinued Drugs				2
1	Tandutinib	Drug Info	Discontinued in Phase 2	Anaplastic mixed oligoastrocytoma
2	SU5614	Drug Info	Terminated	Airway inflammation

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han