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Target
Integrase
Ligand
BDBM50492496
Substrate
n/a
Meas. Tech.
ChEMBL_969976 (CHEMBL2405242)
IC50
3.0±n/a nM
Citation
Johns, BA; Kawasuji, T; Weatherhead, JG; Taishi, T; Temelkoff, DP; Yoshida, H; Akiyama, T; Taoda, Y; Murai, H; Kiyama, R; Fuji, M; Tanimoto, N; Jeffrey, J; Foster, SA; Yoshinaga, T; Seki, T; Kobayashi, M; Sato, A; Johnson, MN; Garvey, EP; Fujiwara, T Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744). J Med Chem 56:5901-16 (2013) [PubMed] Article
More Info.:
Target
Name:
Integrase
Synonyms:
pol
Type:
PROTEIN
Mol. Mass.:
32203.43
Organism:
Human immunodeficiency virus 1
Description:
ChEMBL_106649
Residue:
288
Sequence:
FLDGIDKAQEEHEKYHSNWRAMASDFNLPPVVAKEIVASCDKCQLKGEAMHGQVDCSPGIWQLDCTHLEGKVILVAVHVASGYIEAEVIPAETGQETAYFLLKLAGRWPVKTVHTDNGSNFTSTTVKAACWWAGIKQEFGIPYNPQSQGVIESMNKELKKIIGQVRDQAEHLKTAVQMAVFIHNFKRKGGIGGYSAGERIVDIIATDIQTKELQKQITKIQNFRVYYRDSRDPVWKGPAKLLWKGEGAVVIQDNSDIKVVPRRKAKIIRDYGKQMAGDDCVASRQDED