Reaction Details 
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Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50001580
Substrate
n/a
Meas. Tech.
ChEMBL_1336033 (CHEMBL3240326)
IC50
8.0±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] ArticleMore 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:
BDBM50001580
Synonyms:
CHEMBL3237715
Type:
Small organic molecule
Emp. Form.:
C27H34N8O2S
Mol. Mass.:
534.676
SMILES:
C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc(nn3)N3CCC(CS(C)(=O)=O)CC3)nc12 |r,wU:4.7,wD:1.0,(9.65,-57.17,;9.18,-55.71,;10.22,-54.56,;9.75,-53.09,;8.24,-52.78,;7.21,-53.92,;7.68,-55.38,;7.77,-51.31,;8.68,-50.06,;10.21,-49.91,;10.84,-48.5,;9.93,-47.25,;8.4,-47.41,;7.78,-48.81,;6.31,-49.28,;4.96,-48.52,;3.64,-49.3,;3.65,-50.83,;2.32,-51.6,;2.3,-53.14,;3.62,-53.91,;3.61,-55.44,;2.27,-56.2,;.95,-55.42,;.97,-53.89,;2.26,-57.75,;.92,-58.5,;.9,-60.03,;2.23,-60.82,;2.21,-62.36,;3.53,-63.15,;4.87,-62.4,;2.75,-64.47,;4.29,-64.47,;3.57,-60.07,;3.59,-58.52,;4.98,-51.6,;6.3,-50.83,)|
Structure:
