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Assay Detail

CHEMBL4267922

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

Binding
Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay
18
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 Intermediate

Target

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

Publication

Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
Gu SX, Lu HH, Liu GY, Ju XL, Zhu YY.
Eur J Med Chem (2018) 158 : 371 -392
PubMed 30223123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.19 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70517 1 9.40
CHEMBL312764 1 9.05
CHEMBL308954 ETRAVIRINE 4.0 1 8.92
CHEMBL72528 1 8.89
CHEMBL308004 1 8.77
CHEMBL70442 1 8.72
CHEMBL69890 1 8.59
CHEMBL72335 1 8.57
CHEMBL72242 1 8.48
CHEMBL307950 1 8.24
CHEMBL71881 1 8.21
CHEMBL70514 1 8.00
CHEMBL74239 1 7.92
CHEMBL72652 1 7.41
CHEMBL307297 1 7.40
CHEMBL421112 1 4.48
CHEMBL302360 1 -
CHEMBL74226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70517 IC50 = 0.4 nM 9.40
CHEMBL312764 IC50 = 0.9 nM 9.05
CHEMBL308954 ETRAVIRINE IC50 = 1.2 nM 8.92
CHEMBL72528 IC50 = 1.3 nM 8.89
CHEMBL308004 IC50 = 1.7 nM 8.77
CHEMBL70442 IC50 = 1.9 nM 8.72
CHEMBL69890 IC50 = 2.6 nM 8.59
CHEMBL72335 IC50 = 2.7 nM 8.57
CHEMBL72242 IC50 = 3.3 nM 8.48
CHEMBL307950 IC50 = 5.8 nM 8.24
CHEMBL71881 IC50 = 6.2 nM 8.21
CHEMBL70514 IC50 = 10.0 nM 8.00
CHEMBL74239 IC50 = 12.0 nM 7.92
CHEMBL72652 IC50 = 39.0 nM 7.41
CHEMBL307297 IC50 = 40.0 nM 7.40
CHEMBL421112 IC50 = 33300.0 nM 4.48
CHEMBL302360 IC50 - -
CHEMBL74226 IC50 > 100000.0 nM -