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Assay Detail

CHEMBL1918322

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Binding
Inhibition of HIV1 integrase strand transfer by biochemical assay
22
Total Activities
22
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

Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors.
Johns BA, Kawasuji T, Weatherhead JG, Boros EE, Thompson JB, Garvey EP, Foster SA, Jeffrey JL, Miller WH, Kurose N, Matsumura K, Fujiwara T.
Bioorg Med Chem Lett (2011) 21 : 6461 -6464
PubMed 21945283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.91 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1917873 1 9.00
CHEMBL1914460 1 8.40
CHEMBL1917874 1 8.22
CHEMBL1917876 1 8.22
CHEMBL1914553 1 8.22
CHEMBL1914551 1 8.15
CHEMBL1914564 1 8.10
CHEMBL1914554 1 8.10
CHEMBL1914552 1 8.00
CHEMBL1917875 1 7.89
CHEMBL1917872 1 7.89
CHEMBL1914562 1 7.85
CHEMBL1914556 1 7.77
CHEMBL1914557 1 7.75
CHEMBL1914563 1 7.72
CHEMBL1914555 1 7.70
CHEMBL1914559 1 7.55
CHEMBL1914560 1 7.55
CHEMBL1914550 1 7.50
CHEMBL1914561 1 7.50
CHEMBL1914558 1 7.47
CHEMBL1917877 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1917873 IC50 = 1.0 nM 9.00
CHEMBL1914460 IC50 = 4.0 nM 8.40
CHEMBL1917874 IC50 = 6.0 nM 8.22
CHEMBL1917876 IC50 = 6.0 nM 8.22
CHEMBL1914553 IC50 = 6.0 nM 8.22
CHEMBL1914551 IC50 = 7.0 nM 8.15
CHEMBL1914564 IC50 = 8.0 nM 8.10
CHEMBL1914554 IC50 = 8.0 nM 8.10
CHEMBL1914552 IC50 = 10.0 nM 8.00
CHEMBL1917875 IC50 = 13.0 nM 7.89
CHEMBL1917872 IC50 = 13.0 nM 7.89
CHEMBL1914562 IC50 = 14.0 nM 7.85
CHEMBL1914556 IC50 = 17.0 nM 7.77
CHEMBL1914557 IC50 = 18.0 nM 7.75
CHEMBL1914563 IC50 = 19.0 nM 7.72
CHEMBL1914555 IC50 = 20.0 nM 7.70
CHEMBL1914559 IC50 = 28.0 nM 7.55
CHEMBL1914560 IC50 = 28.0 nM 7.55
CHEMBL1914550 IC50 = 32.0 nM 7.50
CHEMBL1914561 IC50 = 32.0 nM 7.50
CHEMBL1914558 IC50 = 34.0 nM 7.47
CHEMBL1917877 IC50 = 35.0 nM 7.46