| Reaction Details |
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 | Report a problem with these data |
| Target | Receptor-type tyrosine-protein kinase FLT3 |
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| Ligand | BDBM158154 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1577154 (CHEMBL3807416) |
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| IC50 | 164±n/a nM |
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| Citation |  Menichincheri, M; Ardini, E; Magnaghi, P; Avanzi, N; Banfi, P; Bossi, R; Buffa, L; Canevari, G; Ceriani, L; Colombo, M; Corti, L; Donati, D; Fasolini, M; Felder, E; Fiorelli, C; Fiorentini, F; Galvani, A; Isacchi, A; Borgia, AL; Marchionni, C; Nesi, M; Orrenius, C; Panzeri, A; Pesenti, E; Rusconi, L; Saccardo, MB; Vanotti, E; Perrone, E; Orsini, P Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. J Med Chem59:3392-408 (2016) [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 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 112888.62 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P36888 |
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| Residue: | 993 |
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| Sequence: | MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESP
EDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDL
QNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQD
ALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRE
CTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEM
STYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYE
IDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHA
ENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITE
GVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQD
NISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYD
LKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMS
ELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKE
HNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDL
NVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDS
NYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYK
LIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDG
RVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
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| BDBM158154 |
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| n/a |
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| Name | BDBM158154 |
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| Synonyms: | US10081622, Compound 11 | US10370379, Entrectinib | US11059827, Compound Entrectinib | US11267806, Compound T-12 | US9029356, 11 | US9255087, 11 | US9616059, 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C31H34F2N6O2 |
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| Mol. Mass. | 560.6375 |
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| SMILES | CN1CCN(CC1)c1ccc(C(=O)Nc2n[nH]c3ccc(Cc4cc(F)cc(F)c4)cc23)c(NC2CCOCC2)c1 |
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| Structure | 
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