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Assay Detail

CHEMBL801172

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

Binding
In vitro inhibitory activity against HIV-1 wild type reverse transcriptase (RT)
13
Total Activities
13
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

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 13 6.93 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL336441 1 7.68
CHEMBL137838 1 7.66
CHEMBL141223 1 7.52
CHEMBL140665 1 7.22
CHEMBL139532 1 7.16
CHEMBL138969 1 7.03
CHEMBL344257 1 7.00
CHEMBL329653 1 6.72
CHEMBL57 NEVIRAPINE 4.0 1 6.40
CHEMBL342620 1 6.01
CHEMBL141371 1 5.82
CHEMBL423549 1 -
CHEMBL342883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL336441 Ki = 21.0 nM 7.68
CHEMBL137838 Ki = 22.0 nM 7.66
CHEMBL141223 Ki = 30.0 nM 7.52
CHEMBL140665 Ki = 60.0 nM 7.22
CHEMBL139532 Ki = 70.0 nM 7.16
CHEMBL138969 Ki = 93.0 nM 7.03
CHEMBL344257 Ki = 100.0 nM 7.00
CHEMBL329653 Ki = 190.0 nM 6.72
CHEMBL57 NEVIRAPINE Ki = 400.0 nM 6.40
CHEMBL342620 Ki = 970.0 nM 6.01
CHEMBL141371 Ki = 1500.0 nM 5.82
CHEMBL423549 Ki = - nM -
CHEMBL342883 Ki = - nM -