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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM112470
Substrate
n/a
Meas. Tech.
Kinase Assay
pH
7.6±n/a
IC50
73.7±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:
BDBM112470
Synonyms:
US8623885, 11
Type:
Small organic molecule
Emp. Form.:
C24H27N7
Mol. Mass.:
413.5181
SMILES:
C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3cc4CNCCc4cn3)nc12 |r,wU:4.7,wD:1.0,(3.46,-4.37,;3.06,-2.88,;4.15,-1.79,;3.75,-.3,;2.27,.09,;1.18,-.99,;1.58,-2.48,;1.87,1.58,;2.77,2.83,;4.3,2.99,;4.93,4.4,;4.03,5.64,;2.49,5.48,;1.87,4.07,;.4,3.6,;-.93,4.37,;-2.26,3.6,;-2.26,2.06,;-3.6,1.29,;-3.6,-.25,;-2.26,-1.02,;-2.26,-2.56,;-.93,-3.33,;-.93,-4.87,;-2.26,-5.64,;-3.6,-4.87,;-3.6,-3.33,;-4.93,-2.56,;-4.93,-1.02,;-.93,1.29,;.4,2.06,)|
Structure:
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