Reaction Details Report a problem with these data
Target
Receptor-type tyrosine-protein kinase FLT3 [D835Y]
Ligand
BDBM397431
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
<1±n/a nM
Citation
 Naoe, T; Kiyoi, H; Hagiwara, S; Takasaki, M; Hirano, D; Nakatani, T; Yamaura, T Pharmaceutical composition for treating FLT3 mutation-positive cancer, mutant FLT3 inhibitor and uses thereof US Patent  US9987278 Publication Date 6/5/2018 
Target
Name:
Receptor-type tyrosine-protein kinase FLT3 [D835Y]
Synonyms:
CD135 | FL cytokine receptor | FLK2 | FLT3 | FLT3(D835Y) | FLT3_HUMAN | Receptor-type tyrosine-protein kinase FLT3 (D835Y) | STK-1 | STK1 | Stem cell tyrosine kinase 1 | Tyrosine Kinase FLT3 Mutant (D835Y)
Type:
n/a
Mol. Mass.:
112937.71
Organism:
Homo sapiens (Human)
Description:
P36888 D835Y
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARYIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
  
Inhibitor
Name:
BDBM397431
Synonyms:
US9987278, Compound Reference 41
Type:
Small organic molecule
Emp. Form.:
C27H34FN7O2
Mol. Mass.:
507.603
SMILES:
CNc1nc(Nc2ccc(F)cc2)ncc1C#C[C@@H]1C[C@@H](C1)NC(=O)[C@H](C)N(C)C(=O)\C=C\CN(C)C |r,wU:18.19,20.24,25.28,(7.61,1.38,;6.28,.61,;6.28,-.93,;7.61,-1.7,;7.61,-3.24,;8.95,-4.01,;10.28,-3.24,;11.61,-4.01,;12.95,-3.24,;12.95,-1.7,;14.28,-.93,;11.61,-.93,;10.28,-1.7,;6.28,-4.01,;4.94,-3.24,;4.94,-1.7,;3.61,-.93,;2.28,-.16,;.94,.61,;.54,2.1,;-.94,1.7,;-.54,.21,;-2.28,2.47,;-3.61,1.7,;-3.61,.16,;-4.94,2.47,;-4.94,4.01,;-6.28,1.7,;-6.28,.16,;-7.61,2.47,;-7.61,4.01,;-8.95,1.7,;-10.28,2.47,;-11.61,1.7,;-12.95,2.47,;-14.28,1.7,;-12.95,4.01,)|
Structure:
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