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Assay Detail

CHEMBL802885

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Binding
In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution K103N
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
Campiani G, Morelli E, Fabbrini M, Nacci V, Greco G, Novellino E, Ramunno A, Maga G, Spadari S, Caliendo G, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Nacca A, Caccia S.
J Med Chem (1999) 42 : 4462 -4470
PubMed 10543890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.44 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140665 1 7.66
CHEMBL336441 1 7.52
CHEMBL138969 1 7.35
CHEMBL344257 1 7.16
CHEMBL137838 1 6.52
CHEMBL141223 1 6.40
CHEMBL139532 1 5.96
CHEMBL141371 1 5.57
CHEMBL57 NEVIRAPINE 4.0 1 5.16
CHEMBL329653 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140665 Ki = 22.0 nM 7.66
CHEMBL336441 Ki = 30.0 nM 7.52
CHEMBL138969 Ki = 45.0 nM 7.35
CHEMBL344257 Ki = 70.0 nM 7.16
CHEMBL137838 Ki = 300.0 nM 6.52
CHEMBL141223 Ki = 400.0 nM 6.40
CHEMBL139532 Ki = 1100.0 nM 5.96
CHEMBL141371 Ki = 2700.0 nM 5.57
CHEMBL57 NEVIRAPINE Ki = 7000.0 nM 5.16
CHEMBL329653 Ki = 7700.0 nM 5.11