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Assay Detail

CHEMBL800583

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

Binding
Inhibitory activity against HIV-1 reverse transcriptase (RT)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
Saari WS, Hoffman JM, Wai JS, Fisher TE, Rooney CS, Smith AM, Thomas CM, Goldman ME, O'Brien JA, Nunberg JH.
J Med Chem (1991) 34 : 2922 -2925
PubMed 1716683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.92 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99235 1 8.02
CHEMBL268871 L-697661 1 7.72
CHEMBL37803 1 7.70
CHEMBL83622 1 7.66
CHEMBL329720 1 7.64
CHEMBL83825 1 7.52
CHEMBL99992 1 7.26
CHEMBL98159 1 7.11
CHEMBL99018 1 6.90
CHEMBL415320 1 6.68
CHEMBL316785 1 6.63
CHEMBL431274 1 6.46
CHEMBL95426 1 6.43
CHEMBL318730 1 6.36
CHEMBL82439 1 5.43
CHEMBL98394 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99235 IC50 = 9.6 nM 8.02
CHEMBL268871 L-697661 IC50 = 19.0 nM 7.72
CHEMBL37803 IC50 = 20.0 nM 7.70
CHEMBL83622 IC50 = 22.0 nM 7.66
CHEMBL329720 IC50 = 23.0 nM 7.64
CHEMBL83825 IC50 = 30.0 nM 7.52
CHEMBL99992 IC50 = 55.0 nM 7.26
CHEMBL98159 IC50 = 77.0 nM 7.11
CHEMBL99018 IC50 = 125.0 nM 6.90
CHEMBL415320 IC50 = 210.0 nM 6.68
CHEMBL316785 IC50 = 235.0 nM 6.63
CHEMBL431274 IC50 = 350.0 nM 6.46
CHEMBL95426 IC50 = 370.0 nM 6.43
CHEMBL318730 IC50 = 440.0 nM 6.36
CHEMBL82439 IC50 = 3700.0 nM 5.43
CHEMBL98394 IC50 = 6400.0 nM 5.19