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Assay Detail

CHEMBL701160

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Compound was tested for its ability to inhibit the strand transfer of the integration process catalyzed by HIV integrase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Zhuang L, Wai JS, Embrey MW, Fisher TE, Egbertson MS, Payne LS, Guare JP, Vacca JP, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Witmer MV, Moyer G, Schleif WA, Gabryelski LJ, Leonard YM, Lynch JJ, Michelson SR, Young SD.
J Med Chem (2003) 46 : 453 -456
PubMed 12570367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.05 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19464 1 8.00
CHEMBL32865 1 8.00
CHEMBL36070 1 7.40
CHEMBL142072 1 7.30
CHEMBL35842 1 6.43
CHEMBL288097 1 6.22
CHEMBL140319 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19464 IC50 = 10.0 nM 8.00
CHEMBL32865 IC50 = 10.0 nM 8.00
CHEMBL36070 IC50 = 40.0 nM 7.40
CHEMBL142072 IC50 = 50.0 nM 7.30
CHEMBL35842 IC50 = 370.0 nM 6.43
CHEMBL288097 IC50 = 600.0 nM 6.22
CHEMBL140319 IC50 = 1000.0 nM 6.00