Reaction Details |
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Target | Receptor-type tyrosine-protein kinase FLT3 |
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Ligand | BDBM50250180 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1681208 (CHEMBL4031485) |
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EC50 | <10±n/a nM |
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Citation | Wang, A; Li, X; Chen, C; Wu, H; Qi, Z; Hu, C; Yu, K; Wu, J; Liu, J; Liu, X; Hu, Z; Wang, W; Wang, W; Wang, W; Wang, L; Wang, B; Liu, Q; Li, L; Ge, J; Ren, T; Zhang, S; Xia, R; Liu, J; Liu, Q Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML. J Med Chem60:8407-8424 (2017) [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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BDBM50250180 |
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n/a |
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Name | BDBM50250180 |
Synonyms: | CHEMBL4101411 |
Type | Small organic molecule |
Emp. Form. | C31H35N9O4 |
Mol. Mass. | 597.6675 |
SMILES | CC(C)(C)c1cc(NC(=O)Nc2ccc(cc2)-n2nc(-c3ccc(OCCN4CCOCC4)cc3)c3c(N)ncnc23)no1 |
Structure |
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