Reaction Details |
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Target | Receptor-type tyrosine-protein kinase FLT3 |
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Ligand | BDBM298766 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2119094 (CHEMBL4828160) |
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IC50 | 7.9±n/a nM |
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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 Chem64:13524-13539 (2021) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Receptor-type tyrosine-protein kinase FLT3 |
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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: | MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESP
EDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDL
QNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQD
ALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRE
CTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEM
STYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYE
IDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHA
ENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITE
GVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQD
NISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYD
LKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMS
ELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKE
HNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDL
NVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDS
NYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYK
LIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDG
RVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
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BDBM298766 |
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n/a |
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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 |
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