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Assay Detail

CHEMBL702099

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

Binding
IC50 was measured as concentration required to inhibit 50% of HIV-integrase integration
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Three-dimensional quantitative structure-activity relationship (QSAR) of HIV integrase inhibitors: a comparative molecular field analysis (CoMFA) study.
Raghavan K, Buolamwini JK, Fesen MR, Pommier Y, Kohn KW, Weinstein JN.
J Med Chem (1995) 38 : 890 -897
PubMed 7699704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.97 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413552 QUERCETAGETIN 1 7.00
CHEMBL170405 ROBINETIN 1 5.80
CHEMBL164 MYRICETIN 1 5.60
CHEMBL8260 BAICALEIN 2.0 1 5.37
CHEMBL31574 FISETIN 2.0 1 5.07
CHEMBL1159644 1 4.99
CHEMBL50 QUERCETIN 3.0 1 4.87
CHEMBL2029094 1 4.65
CHEMBL151 LUTEOLIN 2.0 1 4.60
CHEMBL353450 1 4.60
CHEMBL312163 RHAMNETIN 1 4.54
CHEMBL28626 MORIN 1 4.50
CHEMBL171315 1 4.42
CHEMBL172350 EUPAFOLIN 1 4.41
CHEMBL150 KAEMPFEROL 1.0 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413552 QUERCETAGETIN IC50 = 100.0 nM 7.00
CHEMBL170405 ROBINETIN IC50 = 1600.0 nM 5.80
CHEMBL164 MYRICETIN IC50 = 2500.0 nM 5.60
CHEMBL8260 BAICALEIN IC50 = 4300.0 nM 5.37
CHEMBL31574 FISETIN IC50 = 8500.0 nM 5.07
CHEMBL1159644 IC50 = 10300.0 nM 4.99
CHEMBL50 QUERCETIN IC50 = 13600.0 nM 4.87
CHEMBL2029094 IC50 = 22500.0 nM 4.65
CHEMBL151 LUTEOLIN IC50 = 25000.0 nM 4.60
CHEMBL353450 IC50 = 25100.0 nM 4.60
CHEMBL312163 RHAMNETIN IC50 = 28700.0 nM 4.54
CHEMBL28626 MORIN IC50 = 31700.0 nM 4.50
CHEMBL171315 IC50 = 38500.0 nM 4.42
CHEMBL172350 EUPAFOLIN IC50 = 39100.0 nM 4.41
CHEMBL150 KAEMPFEROL IC50 = 64700.0 nM 4.19