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Assay Detail

CHEMBL701719

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

Binding
Inhibition of HIV-1 integrase, under 1 uM for the 3''-preprocessing
26
Total Activities
25
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

Developing a dynamic pharmacophore model for HIV-1 integrase.
Carlson HA, Masukawa KM, Rubins K, Bushman FD, Jorgensen WL, Lins RD, Briggs JM, McCammon JA.
J Med Chem (2000) 43 : 2100 -2114
PubMed 10841789 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.57 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63592 1 6.82
CHEMBL177126 2 6.60
CHEMBL441250 1 6.19
CHEMBL431948 1 6.17
CHEMBL53463 DOXORUBICIN 4.0 1 6.05
CHEMBL292992 1 6.05
CHEMBL553067 1 5.96
CHEMBL430786 1 5.92
CHEMBL413552 QUERCETAGETIN 1 5.89
CHEMBL304722 1 5.85
CHEMBL67076 1 5.77
CHEMBL164 MYRICETIN 1 5.70
CHEMBL66953 PURPUROGALLIN 1 5.68
CHEMBL541123 1 5.64
CHEMBL58 MITOXANTRONE 4.0 1 5.42
CHEMBL29898 QUINALIZARIN 1 5.40
CHEMBL6246 ELLAGIC ACID 2.0 1 5.29
CHEMBL324842 ROSMARINIC ACID 1 5.05
CHEMBL67233 1 5.02
CHEMBL67535 1 5.00
CHEMBL286494 HYPERICIN 3.0 1 5.00
CHEMBL68073 1 4.77
CHEMBL216962 1 4.69
CHEMBL66854 1 4.62
CHEMBL284616 CHLOROGENIC ACID 2.0 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63592 IC50 = 150.0 nM 6.82
CHEMBL177126 IC50 = 250.0 nM 6.60
CHEMBL441250 IC50 = 640.0 nM 6.19
CHEMBL431948 IC50 = 680.0 nM 6.17
CHEMBL177126 IC50 = 790.0 nM 6.10
CHEMBL53463 DOXORUBICIN IC50 = 900.0 nM 6.05
CHEMBL292992 IC50 = 900.0 nM 6.05
CHEMBL553067 IC50 = 1100.0 nM 5.96
CHEMBL430786 IC50 = 1200.0 nM 5.92
CHEMBL413552 QUERCETAGETIN IC50 = 1300.0 nM 5.89
CHEMBL304722 IC50 = 1400.0 nM 5.85
CHEMBL67076 IC50 = 1700.0 nM 5.77
CHEMBL164 MYRICETIN IC50 = 2000.0 nM 5.70
CHEMBL66953 PURPUROGALLIN IC50 = 2100.0 nM 5.68
CHEMBL541123 IC50 = 2300.0 nM 5.64
CHEMBL58 MITOXANTRONE IC50 = 3800.0 nM 5.42
CHEMBL29898 QUINALIZARIN IC50 = 4000.0 nM 5.40
CHEMBL6246 ELLAGIC ACID IC50 = 5100.0 nM 5.29
CHEMBL324842 ROSMARINIC ACID IC50 = 9000.0 nM 5.05
CHEMBL67233 IC50 = 9500.0 nM 5.02
CHEMBL286494 HYPERICIN IC50 = 10000.0 nM 5.00
CHEMBL67535 IC50 = 10000.0 nM 5.00
CHEMBL68073 IC50 = 17000.0 nM 4.77
CHEMBL216962 IC50 = 20600.0 nM 4.69
CHEMBL66854 IC50 = 23900.0 nM 4.62
CHEMBL284616 CHLOROGENIC ACID IC50 = 87800.0 nM 4.06