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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50043674
Substrate
n/a
Meas. Tech.
ChEMBL_1445163 (CHEMBL3375415)
IC50
53±n/a nM
Citation
 Xu, Y; Brenning, BG; Kultgen, SG; Foulks, JM; Clifford, A; Lai, S; Chan, A; Merx, S; McCullar, MV; Kanner, SB; Ho, KK Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors. ACS Med Chem Lett 6:63-7 (2015) [PubMed]  Article 
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:
BDBM50043674
Synonyms:
CHEMBL3355550 | US10047093, 8-54 | US10392392, Example 8-54 | US10875864, EX. 8-54 | US9416132, 8-54
Type:
Small organic molecule
Emp. Form.:
C19H19F3N4O
Mol. Mass.:
376.3756
SMILES:
O[C@H]1CC[C@@H](CC1)Nc1ccn2ncc(-c3cccc(c3)C(F)(F)F)c2n1 |r,wU:1.0,wD:4.7,(12.63,-23.03,;13.97,-23.8,;15.3,-23.04,;16.63,-23.8,;16.63,-25.35,;15.3,-26.12,;13.97,-25.34,;17.96,-26.12,;19.3,-25.35,;19.3,-23.81,;20.63,-23.03,;21.95,-23.81,;23.42,-23.33,;24.33,-24.58,;23.42,-25.83,;24.18,-27.16,;23.39,-28.48,;24.15,-29.82,;25.69,-29.84,;26.47,-28.5,;25.71,-27.17,;28.01,-28.51,;28.77,-29.85,;28.79,-27.18,;29.55,-28.51,;21.95,-25.35,;20.63,-26.11,)|
Structure:
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