Reaction Details
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Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM298766
Substrate
n/a
Meas. Tech.
ChEMBL_2119094 (CHEMBL4828160)
IC50
7.9±n/a nM
Citation
McCoull, W; Boyd, S; Brown, MR; Coen, M; Collingwood, O; Davies, NL; Doherty, A; Fairley, G; Goldberg, K; Hardaker, E; He, G; Hennessy, EJ; Hopcroft, P; Hodgson, G; Jackson, A; Jiang, X; Karmokar, A; Lainé, AL; Lindsay, N; Mao, Y; Markandu, R; McMurray, L; McLean, N; Mooney, L; Musgrove, H; Nissink, JWM; Pflug, A; Reddy, VP; Rawlins, PB; Rivers, E; Schimpl, M; Smith, GF; Tentarelli, S; Travers, J; Troup, RI; Walton, J; Wang, C; Wilkinson, S; Williamson, B; Winter-Holt, J; Yang, D; Zheng, Y; Zhu, Q; Smith, PD Optimization of an Imidazo[1,2- J Med Chem 64:13524-13539 (2021) [PubMed] Article More Info.:
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:
Human
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
Inhibitor
Name:
BDBM298766
Synonyms:
2-amino-5-(1-methyl-1H-pyrazol-4-yl)-N-((1S,2S)-2-((4′-((4-methylpiperazin-1-yl)methyl)-[1,1′-biphenyl]-4-yl)methoxy)cyclopentyl)nicotinamide | US10125118, Example 172 | US10947215, Example 172
Type:
Small organic molecule
Emp. Form.:
C34H41N7O2
Mol. Mass.:
579.735
SMILES:
CN1CCN(Cc2ccc(cc2)-c2ccc(CO[C@H]3CCC[C@@H]3NC(=O)c3cc(cnc3N)-c3cnn(C)c3)cc2)CC1 |r|
Structure:
