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Assay Detail

CHEMBL1930122

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

Binding
Inhibition of Human immunodeficiency virus reverse transcriptase K103N mutant by SPA assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.
Gomez R, Jolly S, Williams T, Tucker T, Tynebor R, Vacca J, McGaughey G, Lai MT, Felock P, Munshi V, DeStefano D, Touch S, Miller M, Yan Y, Sanchez R, Liang Y, Paton B, Wan BL, Anthony N.
Bioorg Med Chem Lett (2011) 21 : 7344 -7350
PubMed 22071300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.67 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489586 1 9.41
CHEMBL1928648 1 9.32
CHEMBL1928645 1 8.82
CHEMBL1928646 1 8.80
CHEMBL1928647 1 8.68
CHEMBL1928643 1 8.43
CHEMBL1928644 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489586 Ki = 0.39 nM 9.41
CHEMBL1928648 Ki = 0.48 nM 9.32
CHEMBL1928645 Ki = 1.5 nM 8.82
CHEMBL1928646 Ki = 1.6 nM 8.80
CHEMBL1928647 Ki = 2.1 nM 8.68
CHEMBL1928643 Ki = 3.7 nM 8.43
CHEMBL1928644 Ki = 58.0 nM 7.24