Target
Microtubule-associated protein tau
Ligand
BDBM50586972
Substrate
n/a
Meas. Tech.
ChEMBL_2170288 (CHEMBL5055347)
IC50
4.9±n/a nM
Citation
 Kroth, HOden, FSerra, AMMolette, JMueller, ABerndt, MCapotosti, FGabellieri, ESchmitt-Willich, HHickman, DPfeifer, ADinkelborg, LStephens, A Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core. Bioorg Med Chem 52:0 (2021) [PubMed]  Article 
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:
BDBM50586972
Synonyms:
CHEMBL5088921
Type:
Small organic molecule
Emp. Form.:
C15H9FN4
Mol. Mass.:
264.2572
SMILES:
Fc1cc(ccn1)-c1ccc2c(n1)[nH]c1ccncc21
Structure:
Search PDB for entries with ligand similarity: