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Assay Detail

CHEMBL804264

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

Binding
Inhibition of HIV-1 reverse transcriptase at 37 degree Centigrade
20
Total Activities
20
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

Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.
Rizzo RC, Tirado-Rives J, Jorgensen WL.
J Med Chem (2001) 44 : 145 -154
PubMed 11170624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.72 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39015 1 8.57
CHEMBL276108 1 8.57
CHEMBL35033 EMIVIRINE 2.0 1 8.40
CHEMBL288688 1 8.23
CHEMBL38711 1 7.92
CHEMBL16684 1 7.89
CHEMBL36995 1 7.72
CHEMBL37067 1 7.06
CHEMBL39093 1 7.00
CHEMBL275599 1 6.58
CHEMBL37743 1 6.48
CHEMBL288728 1 5.92
CHEMBL39047 1 5.68
CHEMBL38768 1 5.66
CHEMBL40091 1 5.44
CHEMBL31871 HEPT 1 5.16
CHEMBL36427 1 4.64
CHEMBL286769 1 4.07
CHEMBL290413 1 -
CHEMBL290685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39015 EC50 = 2.7 nM 8.57
CHEMBL276108 EC50 = 2.7 nM 8.57
CHEMBL35033 EMIVIRINE EC50 = 4.0 nM 8.40
CHEMBL288688 EC50 = 5.9 nM 8.23
CHEMBL38711 EC50 = 12.0 nM 7.92
CHEMBL16684 EC50 = 13.0 nM 7.89
CHEMBL36995 EC50 = 19.0 nM 7.72
CHEMBL37067 EC50 = 88.0 nM 7.06
CHEMBL39093 EC50 = 100.0 nM 7.00
CHEMBL275599 EC50 = 260.0 nM 6.58
CHEMBL37743 EC50 = 330.0 nM 6.48
CHEMBL288728 EC50 = 1200.0 nM 5.92
CHEMBL39047 EC50 = 2100.0 nM 5.68
CHEMBL38768 EC50 = 2200.0 nM 5.66
CHEMBL40091 EC50 = 3600.0 nM 5.44
CHEMBL31871 HEPT EC50 = 7000.0 nM 5.16
CHEMBL36427 EC50 = 23000.0 nM 4.64
CHEMBL286769 EC50 = 85000.0 nM 4.07
CHEMBL290413 EC50 > 250000.0 nM -
CHEMBL290685 EC50 > 150000.0 nM -