Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1227437

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

Binding
Inhibition of HIV 1 recombinant integrase
15
Total Activities
15
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 Autocuration

Target

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

Publication

Development of 2-pyrrolidinyl-N-methyl pyrimidones as potent and orally bioavailable HIV integrase inhibitors.
Ferrara M, Fiore F, Summa V, Gardelli C.
Bioorg Med Chem Lett (2010) 20 : 5031 -5034
PubMed 20674351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.79 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1223541 1 8.05
CHEMBL1223401 1 8.00
CHEMBL1223471 1 8.00
CHEMBL1223470 1 8.00
CHEMBL1223542 1 8.00
CHEMBL1223469 1 7.82
CHEMBL1223472 1 7.82
CHEMBL1222461 1 7.72
CHEMBL1223400 1 7.70
CHEMBL1222460 1 7.70
CHEMBL1223543 1 7.68
CHEMBL388908 1 7.64
CHEMBL1223544 1 7.62
CHEMBL1222458 1 7.57
CHEMBL1222459 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1223541 IC50 = 9.0 nM 8.05
CHEMBL1223401 IC50 = 10.0 nM 8.00
CHEMBL1223471 IC50 = 10.0 nM 8.00
CHEMBL1223470 IC50 = 10.0 nM 8.00
CHEMBL1223542 IC50 = 10.0 nM 8.00
CHEMBL1223469 IC50 = 15.0 nM 7.82
CHEMBL1223472 IC50 = 15.0 nM 7.82
CHEMBL1222461 IC50 = 19.0 nM 7.72
CHEMBL1223400 IC50 = 20.0 nM 7.70
CHEMBL1222460 IC50 = 20.0 nM 7.70
CHEMBL1223543 IC50 = 21.0 nM 7.68
CHEMBL388908 IC50 = 23.0 nM 7.64
CHEMBL1223544 IC50 = 24.0 nM 7.62
CHEMBL1222458 IC50 = 27.0 nM 7.57
CHEMBL1222459 IC50 = 32.0 nM 7.50