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Assay Detail

CHEMBL797523

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

Binding
In vitro for inhibition of HIV-1 reverse transcriptase.
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 Expert

Target

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

Publication

Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones.
Proudfoot JR, Patel UR, Kapadia SR, Hargrave KD.
J Med Chem (1995) 38 : 1406 -1410
PubMed 7537334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.46 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343883 1 7.16
CHEMBL57 NEVIRAPINE 4.0 1 7.08
CHEMBL144820 1 7.05
CHEMBL317130 1 6.89
CHEMBL37343 1 6.89
CHEMBL2114381 1 6.82
CHEMBL2115336 1 6.72
CHEMBL70850 1 6.62
CHEMBL2115325 1 6.55
CHEMBL2115328 1 6.54
CHEMBL2115335 1 6.26
CHEMBL39950 1 6.12
CHEMBL2115334 1 6.12
CHEMBL305041 1 6.00
CHEMBL2115323 1 6.00
CHEMBL2115326 1 5.89
CHEMBL298243 1 5.89
CHEMBL2115322 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343883 IC50 = 70.0 nM 7.16
CHEMBL57 NEVIRAPINE IC50 = 84.0 nM 7.08
CHEMBL144820 IC50 = 90.0 nM 7.05
CHEMBL317130 IC50 = 130.0 nM 6.89
CHEMBL37343 IC50 = 130.0 nM 6.89
CHEMBL2114381 IC50 = 150.0 nM 6.82
CHEMBL2115336 IC50 = 190.0 nM 6.72
CHEMBL70850 IC50 = 240.0 nM 6.62
CHEMBL2115325 IC50 = 280.0 nM 6.55
CHEMBL2115328 IC50 = 290.0 nM 6.54
CHEMBL2115335 IC50 = 550.0 nM 6.26
CHEMBL39950 IC50 = 760.0 nM 6.12
CHEMBL2115334 IC50 = 760.0 nM 6.12
CHEMBL305041 IC50 = 1000.0 nM 6.00
CHEMBL2115323 IC50 = 1000.0 nM 6.00
CHEMBL2115326 IC50 = 1300.0 nM 5.89
CHEMBL298243 IC50 = 1300.0 nM 5.89
CHEMBL2115322 IC50 = 1760.0 nM 5.75