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Assay Detail

CHEMBL701899

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

Binding
Inhibition of recombinant HIV-1 Integrase in strand transfer enzyme assay.
21
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Wai JS, Egbertson MS, Payne LS, Fisher TE, Embrey MW, Tran LO, Melamed JY, Langford HM, Guare JP, Zhuang L, Grey VE, Vacca JP, Holloway MK, Naylor-Olsen AM, Hazuda DJ, Felock PJ, Wolfe AL, Stillmock KA, Schleif WA, Gabryelski LJ, Young SD.
J Med Chem (2000) 43 : 4923 -4926
PubMed 11150161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.47 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143614 2 7.00
CHEMBL147317 1 6.85
CHEMBL146777 1 6.82
CHEMBL50605 1 6.77
CHEMBL359212 1 6.75
CHEMBL342295 1 6.66
CHEMBL144727 1 6.60
CHEMBL358506 1 6.30
CHEMBL144118 2 6.30
CHEMBL145946 2 6.30
CHEMBL147209 1 5.25
CHEMBL145280 1 -
CHEMBL147147 1 -
CHEMBL148241 1 -
CHEMBL357909 1 -
CHEMBL145705 1 -
CHEMBL19464 1 -
CHEMBL145335 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143614 IC50 = 100.0 nM 7.00
CHEMBL147317 IC50 = 140.0 nM 6.85
CHEMBL146777 IC50 = 150.0 nM 6.82
CHEMBL143614 IC50 = 160.0 nM 6.80
CHEMBL50605 IC50 = 170.0 nM 6.77
CHEMBL359212 IC50 = 180.0 nM 6.75
CHEMBL342295 IC50 = 220.0 nM 6.66
CHEMBL144727 IC50 = 250.0 nM 6.60
CHEMBL358506 IC50 = 500.0 nM 6.30
CHEMBL144118 IC50 = 500.0 nM 6.30
CHEMBL145946 IC50 = 500.0 nM 6.30
CHEMBL145946 IC50 = 600.0 nM 6.22
CHEMBL144118 IC50 = 1000.0 nM 6.00
CHEMBL147209 IC50 = 5670.0 nM 5.25
CHEMBL147147 IC50 < 100.0 nM -
CHEMBL145280 IC50 < 100.0 nM -
CHEMBL148241 IC50 < 100.0 nM -
CHEMBL357909 IC50 < 100.0 nM -
CHEMBL145705 IC50 < 100.0 nM -
CHEMBL19464 IC50 < 100.0 nM -
CHEMBL145335 IC50 < 100.0 nM -