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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50001543
Substrate
n/a
Meas. Tech.
ChEMBL_1336033 (CHEMBL3240326)
IC50
1.000000±n/a nM
Citation
Li, Z; Wang, X; Eksterowicz, J; Gribble, MW; Alba, GQ; Ayres, M; Carlson, TJ; Chen, A; Chen, X; Cho, R; Connors, RV; DeGraffenreid, M; Deignan, JT; Duquette, J; Fan, P; Fisher, B; Fu, J; Huard, JN; Kaizerman, J; Keegan, KS; Li, C; Li, K; Li, Y; Liang, L; Liu, W; Lively, SE; Lo, MC; Ma, J; McMinn, DL; Mihalic, JT; Modi, K; Ngo, R; Pattabiraman, K; Piper, DE; Queva, C; Ragains, ML; Suchomel, J; Thibault, S; Walker, N; Wang, X; Wang, Z; Wanska, M; Wehn, PM; Weidner, MF; Zhang, AJ; Zhao, X; Kamb, A; Wickramasinghe, D; Dai, K; McGee, LR; Medina, JC Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. J Med Chem 57:3430-49 (2014) [PubMed] Article
More Info.:
Target
Name:
Receptor-type tyrosine-protein kinase FLT3
Synonyms:
CD135 | CD_antigen: CD135 | FL cytokine receptor | FLK-2 | FLK2 | FLT-3 | FLT3 | FLT3_HUMAN | Fetal liver kinase-2 | Fms-like tyrosine kinase 3 | Fms-like tyrosine kinase 3 (Flt-3) | Fms-related tyrosine kinase 3 | STK-1 | STK1 | Stem cell tyrosine kinase 1
Type:
Enzyme
Mol. Mass.:
112888.62
Organism:
Homo sapiens (Human)
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
Inhibitor
Name:
BDBM50001543
Synonyms:
CHEMBL3237708
Type:
Small organic molecule
Emp. Form.:
C26H32N8
Mol. Mass.:
456.5859
SMILES:
C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc(cn3)N3CCC(N)CC3)nc12 |r,wU:4.7,wD:1.0,(11.29,-49.99,;10.82,-48.52,;11.85,-47.38,;11.38,-45.91,;9.88,-45.59,;8.84,-46.74,;9.31,-48.2,;9.41,-44.13,;10.31,-42.88,;11.84,-42.73,;12.48,-41.32,;11.56,-40.07,;10.04,-40.23,;9.41,-41.63,;7.94,-42.1,;6.6,-41.34,;5.27,-42.12,;5.28,-43.65,;3.95,-44.42,;3.96,-45.96,;5.29,-46.72,;5.3,-48.25,;3.96,-49.03,;2.63,-48.27,;2.62,-46.73,;3.97,-50.58,;2.64,-51.35,;2.64,-52.89,;3.98,-53.66,;3.98,-55.2,;5.31,-52.88,;5.31,-51.34,;6.62,-44.42,;7.94,-43.65,)|