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Target
Microtubule-associated protein tau
Ligand
BDBM50613246
Substrate
n/a
Meas. Tech.
ChEMBL_2291542
IC50
86±n/a nM
Citation
 Hartz, RA; Ahuja, VT; Sivaprakasam, P; Xiao, H; Krause, CM; Clarke, WJ; Kish, K; Lewis, H; Szapiel, N; Ravirala, R; Mutalik, S; Nakmode, D; Shah, D; Burton, CR; Macor, JE; Dubowchik, GM Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2- J Med Chem 66:4231-4252 (2023) [PubMed] 
Target
Name:
Microtubule-associated protein tau
Synonyms:
MAPT | MAPTL | MTBT1 | Microtubule-associated protein tau | Neurofibrillary tangle protein | PHF-tau | Paired helical filament-tau | TAU | TAU_HUMAN | Tau Protein
Type:
Protein
Mol. Mass.:
78928.63
Organism:
Homo sapiens (Human)
Description:
P10636
Residue:
758
Sequence:
MAEPRQEFEVMEDHAGTYGLGDRKDQGGYTMHQDQEGDTDAGLKESPLQTPTEDGSEEPGSETSDAKSTPTAEDVTAPLVDEGAPGKQAAAQPHTEIPEGTTAEEAGIGDTPSLEDEAAGHVTQEPESGKVVQEGFLREPGPPGLSHQLMSGMPGAPLLPEGPREATRQPSGTGPEDTEGGRHAPELLKHQLLGDLHQEGPPLKGAGGKERPGSKEEVDEDRDVDESSPQDSPPSKASPAQDGRPPQTAAREATSIPGFPAEGAIPLPVDFLSKVSTEIPASEPDGPSVGRAKGQDAPLEFTFHVEITPNVQKEQAHSEEHLGRAAFPGAPGEGPEARGPSLGEDTKEADLPEPSEKQPAAAPRGKPVSRVPQLKARMVSKSKDGTGSDDKKAKTSTRSSAKTLKNRPCLSPKHPTPGSSDPLIQPSSPAVCPEPPSSPKYVSSVTSRTGSSGAKEMKLKGADGKTKIATPRGAAPPGQKGQANATRIPAKTPPAPKTPPSSGEPPKSGDRSGYSSPGSPGTPGSRSRTPSLPTPPTREPKKVAVVRTPPKSPSSAKSRLQTAPVPMPDLKNVKSKIGSTENLKHQPGGGKVQIINKKLDLSNVQSKCGSKDNIKHVPGGGSVQIVYKPVDLSKVTSKCGSLGNIHHKPGGGQVEVKSEKLDFKDRVQSKIGSLDNITHVPGGGNKKIETHKLTFRENAKAKTDHGAEIVYKSPVVSGDTSPRHLSNVSSTGSIDMVDSPQLATLADEVSASLAKQGL
  
Inhibitor
Name:
BDBM50613246
Synonyms:
CHEMBL5316226
Type:
Small organic molecule
Emp. Form.:
C23H22N6O2
Mol. Mass.:
414.4598
SMILES:
C[C@@H]1CN(CCO1)c1ccncc1NC(=O)c1ccnn2cc(nc12)-c1ccccc1 |r|
Structure:
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