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Assay Detail

CHEMBL701793

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

Binding
Inhibitory concentration of compound against disintegration (reversal of strand transfer)of HIV-1 integrase
8
Total Activities
8
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 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Depsides and depsidones as inhibitors of HIV-1 integrase: discovery of novel inhibitors through 3D database searching.
Neamati N, Hong H, Mazumder A, Wang S, Sunder S, Nicklaus MC, Milne GW, Proksa B, Pommier Y.
J Med Chem (1997) 40 : 942 -951
PubMed 9083483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.60 4.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL173530 STICTIC ACID 1 4.93
CHEMBL285415 1 4.89
CHEMBL177021 1 4.58
CHEMBL171637 PHYSODIC ACID 1 4.49
CHEMBL366410 1 4.47
CHEMBL171896 1 4.46
CHEMBL172018 1 4.41
CHEMBL367881 (+)-USNIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL173530 STICTIC ACID IC50 = 11700.0 nM 4.93
CHEMBL285415 IC50 = 12800.0 nM 4.89
CHEMBL177021 IC50 = 26000.0 nM 4.58
CHEMBL171637 PHYSODIC ACID IC50 = 32500.0 nM 4.49
CHEMBL366410 IC50 = 33500.0 nM 4.47
CHEMBL171896 IC50 = 35000.0 nM 4.46
CHEMBL172018 IC50 = 39000.0 nM 4.41
CHEMBL367881 (+)-USNIC ACID IC50 = 133000.0 nM -