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Assay Detail

CHEMBL1805161

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Binding
Inhibition of HIV1 reverse transcriptase L100I mutant/poly(rA)/oligo(dT) DNA/dTTP ternary complex
3
Total Activities
3
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 Autocuration

Target

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

Publication

Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
Butini S, Gemma S, Brindisi M, Borrelli G, Fiorini I, Samuele A, Karytinos A, Facchini M, Lossani A, Zanoli S, Campiani G, Novellino E, Focher F, Maga G.
Bioorg Med Chem Lett (2011) 21 : 3935 -3938
PubMed 21636271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.88 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1688505 1 7.52
CHEMBL1688575 1 6.82
CHEMBL1688496 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1688505 Ki = 30.0 nM 7.52
CHEMBL1688575 Ki = 150.0 nM 6.82
CHEMBL1688496 Ki = 510.0 nM 6.29