Reaction Details |
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Target | Receptor-type tyrosine-protein kinase FLT3 |
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Ligand | BDBM50401438 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_883356 (CHEMBL2214092) |
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Kd | 5.4±n/a nM |
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Citation | Bavetsias, V; Crumpler, S; Sun, C; Avery, S; Atrash, B; Faisal, A; Moore, AS; Kosmopoulou, M; Brown, N; Sheldrake, PW; Bush, K; Henley, A; Box, G; Valenti, M; de Haven Brandon, A; Raynaud, FI; Workman, P; Eccles, SA; Bayliss, R; Linardopoulos, S; Blagg, J Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia. J Med Chem55:8721-34 (2012) [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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BDBM50401438 |
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n/a |
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Name | BDBM50401438 |
Synonyms: | CHEMBL2203775 |
Type | Small organic molecule |
Emp. Form. | C26H31ClN8O |
Mol. Mass. | 507.03 |
SMILES | CN1CCN(CC1)c1cccc(c1)-c1nc2ncc(Cl)c(N3CCN(Cc4cc(C)on4)CC3)c2[nH]1 |
Structure |
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