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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM112479
Substrate
n/a
Meas. Tech.
Kinase Assay
pH
7.6±n/a
IC50
144±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:
BDBM112479
Synonyms:
US8623885, 20
Type:
Small organic molecule
Emp. Form.:
C27H31N7O3
Mol. Mass.:
501.5801
SMILES:
COc1cc2c(cn1)n([C@H]1CC[C@H](C)CC1)c1nc(Nc3ccc4CN(CCc4n3)C(=O)CO)ncc21 |r,wU:9.9,wD:12.13,(4.41,8.12,;5.32,6.88,;4.69,5.47,;3.16,5.31,;2.53,3.9,;3.44,2.66,;4.97,2.82,;5.6,4.22,;2.53,1.41,;2.93,-.08,;4.42,-.48,;4.82,-1.96,;3.73,-3.05,;4.13,-4.54,;2.24,-2.65,;1.84,-1.17,;1.07,1.89,;-.26,1.12,;-1.6,1.89,;-2.93,1.12,;-2.93,-.42,;-1.6,-1.19,;-1.6,-2.73,;-2.93,-3.5,;-2.93,-5.04,;-4.26,-5.81,;-5.6,-5.04,;-5.6,-3.5,;-4.26,-2.73,;-4.26,-1.19,;-4.26,-7.35,;-5.6,-8.12,;-2.93,-8.12,;-1.6,-7.35,;-1.6,3.43,;-.26,4.2,;1.07,3.43,)|
Structure:
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