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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM112466
Substrate
n/a
Meas. Tech.
Kinase Assay
pH
7.6±n/a
IC50
21.4±n/a nM
Citation
 Chen, X; Dai, K; Duquette, J; Gribble, Jr., MW; Huard, JN; Keegan, KS; Li, Z; Lively, SE; McGee, LR; Ragains, ML; Wang, X; Weidner, MF; Zhang, J Fused tricyclic dual inhibitors of CDK 4/6 and FLT3 US Patent  US8623885 Publication Date 1/7/2014
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:
BDBM112466
Synonyms:
US8623885, 7
Type:
Small organic molecule
Emp. Form.:
C27H30F3N7
Mol. Mass.:
509.5692
SMILES:
C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc4CN(CCC(F)(F)F)CCc4n3)nc12 |r,wU:4.7,wD:1.0,(4.13,-2.93,;3.73,-1.44,;4.82,-.35,;4.42,1.13,;2.93,1.53,;1.84,.44,;2.24,-1.04,;2.53,3.02,;3.44,4.26,;4.97,4.43,;5.6,5.83,;4.69,7.08,;3.16,6.92,;2.53,5.51,;1.07,5.03,;-.26,5.8,;-1.6,5.03,;-1.6,3.49,;-2.93,2.72,;-2.93,1.18,;-1.6,.41,;-1.6,-1.13,;-2.93,-1.9,;-2.93,-3.44,;-4.26,-4.21,;-4.26,-5.75,;-2.93,-6.52,;-2.93,-8.06,;-2.93,-9.6,;-4.47,-8.06,;-1.39,-8.06,;-5.6,-3.44,;-5.6,-1.9,;-4.26,-1.13,;-4.26,.41,;-.26,2.72,;1.07,3.49,)|
Structure:
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