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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50328414
Substrate
n/a
Meas. Tech.
ChEMBL_665527 (CHEMBL1261358)
IC50
98±n/a nM
Citation
Chen, CH; Lee, O; Yao, CN; Chuang, MY; Chang, YL; Chang, MH; Wen, YF; Yang, WH; Ko, CH; Chou, NT; Lin, MW; Lai, CP; Sun, CY; Wang, LM; Chen, YC; Hseu, TH; Chang, CN; Hsu, HC; Lin, HC; Chang, YL; Shih, YC; Chou, SH; Hsu, YL; Tseng, HW; Liu, CP; Tu, CM; Hu, TL; Tsai, YJ; Chen, TS; Lin, CL; Chiou, SJ; Liu, CC; Hwang, CS Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett 20:6129-32 (2010) [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:
Homo sapiens (Human)
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
Inhibitor
Name:
BDBM50328414
Synonyms:
CHEMBL1258603 | E/Z-(S)-5-fluoro-3-((4-(2-(2-(hydroxymethyl)pyrrolidin-1-yl)ethoxy)-3-methylazulen-1-yl)methylene)indolin-2-one
Type:
Small organic molecule
Emp. Form.:
C27H27FN2O3
Mol. Mass.:
446.5133
SMILES:
Cc1cc(C=C2C(=O)Nc3ccc(F)cc23)c2ccccc(OCCN3CCC[C@H]3CO)c12 |r,w:4.3|