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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM112478
Substrate
n/a
Meas. Tech.
Kinase Assay
pH
7.6±n/a
IC50
33±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:
BDBM112478
Synonyms:
US8623885, 19
Type:
Small organic molecule
Emp. Form.:
C25H29N7O
Mol. Mass.:
443.5441
SMILES:
COc1cc2c(cn1)n([C@H]1CC[C@H](C)CC1)c1nc(Nc3ccc4CNCCc4n3)ncc21 |r,wU:9.9,wD:12.13,(4.41,6.97,;5.32,5.72,;4.69,4.32,;3.16,4.15,;2.53,2.75,;3.44,1.5,;4.97,1.66,;5.6,3.07,;2.53,.26,;2.93,-1.23,;4.42,-1.63,;4.82,-3.12,;3.73,-4.21,;4.13,-5.69,;2.24,-3.81,;1.84,-2.32,;1.07,.73,;-.26,-.04,;-1.6,.73,;-2.93,-.04,;-2.93,-1.58,;-1.6,-2.35,;-1.6,-3.89,;-2.93,-4.66,;-2.93,-6.2,;-4.26,-6.97,;-5.6,-6.2,;-5.6,-4.66,;-4.26,-3.89,;-4.26,-2.35,;-1.6,2.27,;-.26,3.04,;1.07,2.27,)|
Structure:
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