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Assay Detail

CHEMBL869776

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

Binding
Inhibition of strand transfer activity in HIV1 integrase
8
Total Activities
8
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 integrase (CHEMBL3471)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.
Metobo SE, Jin H, Tsiang M, Kim CU.
Bioorg Med Chem Lett (2006) 16 : 3985 -3988
PubMed 16723226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.74 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212213 1 8.14
CHEMBL212982 1 7.48
CHEMBL209440 1 7.30
CHEMBL386055 1 7.03
CHEMBL209488 1 6.68
CHEMBL214371 1 6.59
CHEMBL380034 1 6.07
CHEMBL214066 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212213 IC50 = 7.2 nM 8.14
CHEMBL212982 IC50 = 33.0 nM 7.48
CHEMBL209440 IC50 = 50.0 nM 7.30
CHEMBL386055 IC50 = 93.0 nM 7.03
CHEMBL209488 IC50 = 210.0 nM 6.68
CHEMBL214371 IC50 = 255.0 nM 6.59
CHEMBL380034 IC50 = 850.0 nM 6.07
CHEMBL214066 IC50 = 24000.0 nM 4.62