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Assay Detail

CHEMBL894312

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

Functional
Antiviral activity against HIV1 with RT L100I mutation by cytopathic cell killing assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
Morningstar ML, Roth T, Farnsworth DW, Smith MK, Watson K, Buckheit RW, Das K, Zhang W, Arnold E, Julias JG, Hughes SH, Michejda CJ.
J Med Chem (2007) 50 : 4003 -4015
PubMed 17663538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.47 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292831 1 7.70
CHEMBL58007 1 7.17
CHEMBL57770 1 7.10
CHEMBL294004 1 7.10
CHEMBL292923 1 6.80
CHEMBL293961 1 6.52
CHEMBL291505 1 6.52
CHEMBL61352 1 6.30
CHEMBL57 NEVIRAPINE 4.0 1 6.14
CHEMBL293984 1 5.92
CHEMBL58494 1 5.78
CHEMBL418637 1 5.61
CHEMBL58358 1 5.49
CHEMBL56435 1 -
CHEMBL59448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292831 EC50 = 20.0 nM 7.70
CHEMBL58007 EC50 = 68.0 nM 7.17
CHEMBL57770 EC50 = 80.0 nM 7.10
CHEMBL294004 EC50 = 80.0 nM 7.10
CHEMBL292923 EC50 = 160.0 nM 6.80
CHEMBL293961 EC50 = 300.0 nM 6.52
CHEMBL291505 EC50 = 300.0 nM 6.52
CHEMBL61352 EC50 = 500.0 nM 6.30
CHEMBL57 NEVIRAPINE EC50 = 720.0 nM 6.14
CHEMBL293984 EC50 = 1200.0 nM 5.92
CHEMBL58494 EC50 = 1660.0 nM 5.78
CHEMBL418637 EC50 = 2480.0 nM 5.61
CHEMBL58358 EC50 = 3250.0 nM 5.49
CHEMBL56435 EC50 - -
CHEMBL59448 EC50 - -