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Assay Detail

CHEMBL1033786

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Binding
Inhibition of HIV1 integrase strand transfer activity
52
Total Activities
52
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

Quinolone carboxylic acids as a novel monoketo acid class of human immunodeficiency virus type 1 integrase inhibitors.
Sato M, Kawakami H, Motomura T, Aramaki H, Matsuda T, Yamashita M, Ito Y, Matsuzaki Y, Yamataka K, Ikeda S, Shinkai H.
J Med Chem (2009) 52 : 4869 -4882
PubMed 19719237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.52 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203443 1 8.05
CHEMBL549549 1 7.92
CHEMBL550893 1 7.68
CHEMBL379664 1 7.62
CHEMBL549546 1 7.60
CHEMBL562360 1 7.58
CHEMBL561099 1 7.51
CHEMBL558481 1 7.50
CHEMBL560439 1 7.47
CHEMBL563162 1 7.46
CHEMBL561100 1 7.42
CHEMBL549611 1 7.39
CHEMBL559903 1 7.37
CHEMBL550895 1 7.36
CHEMBL242883 1 7.30
CHEMBL549750 1 7.30
CHEMBL551437 1 7.26
CHEMBL561827 1 7.19
CHEMBL560234 1 7.16
CHEMBL558286 1 7.11
CHEMBL558287 1 7.08
CHEMBL550691 1 7.08
CHEMBL551235 1 6.94
CHEMBL561437 1 6.67
CHEMBL549405 1 6.60
CHEMBL559705 1 6.43
CHEMBL559704 1 6.39
CHEMBL561423 1 6.30
CHEMBL554504 1 6.17
CHEMBL549338 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203443 IC50 = 9.0 nM 8.05
CHEMBL549549 IC50 = 12.0 nM 7.92
CHEMBL550893 IC50 = 21.0 nM 7.68
CHEMBL379664 IC50 = 24.0 nM 7.62
CHEMBL549546 IC50 = 25.0 nM 7.60
CHEMBL562360 IC50 = 26.0 nM 7.58
CHEMBL561099 IC50 = 31.0 nM 7.51
CHEMBL558481 IC50 = 32.0 nM 7.50
CHEMBL560439 IC50 = 34.0 nM 7.47
CHEMBL563162 IC50 = 35.0 nM 7.46
CHEMBL561100 IC50 = 38.0 nM 7.42
CHEMBL549611 IC50 = 41.0 nM 7.39
CHEMBL559903 IC50 = 43.0 nM 7.37
CHEMBL550895 IC50 = 44.0 nM 7.36
CHEMBL549750 IC50 = 50.0 nM 7.30
CHEMBL242883 IC50 = 50.0 nM 7.30
CHEMBL551437 IC50 = 55.0 nM 7.26
CHEMBL561827 IC50 = 65.0 nM 7.19
CHEMBL560234 IC50 = 70.0 nM 7.16
CHEMBL558286 IC50 = 77.0 nM 7.11
CHEMBL558287 IC50 = 84.0 nM 7.08
CHEMBL550691 IC50 = 83.0 nM 7.08
CHEMBL551235 IC50 = 116.0 nM 6.94
CHEMBL561437 IC50 = 215.0 nM 6.67
CHEMBL549405 IC50 = 250.0 nM 6.60
CHEMBL559705 IC50 = 370.0 nM 6.43
CHEMBL559704 IC50 = 410.0 nM 6.39
CHEMBL561423 IC50 = 500.0 nM 6.30
CHEMBL554504 IC50 = 674.0 nM 6.17
CHEMBL549338 IC50 = 720.0 nM 6.14
CHEMBL560960 IC50 = 800.0 nM 6.10
CHEMBL560761 IC50 = 1080.0 nM 5.97
CHEMBL549404 IC50 = 1170.0 nM 5.93
CHEMBL382680 IC50 = 1630.0 nM 5.79
CHEMBL557480 IC50 = 2300.0 nM 5.64
CHEMBL561619 IC50 = 5600.0 nM 5.25
CHEMBL550080 IC50 = 5800.0 nM 5.24
CHEMBL550220 IC50 = 5800.0 nM 5.24
CHEMBL565125 IC50 = 6000.0 nM 5.22
CHEMBL560836 IC50 = 6700.0 nM 5.17
CHEMBL563677 IC50 = 8200.0 nM 5.09
CHEMBL549816 IC50 = 9000.0 nM 5.05
CHEMBL557891 IC50 = 9800.0 nM 5.01
CHEMBL408699 IC50 = 14400.0 nM 4.84
CHEMBL563525 IC50 = 14800.0 nM 4.83
CHEMBL554722 IC50 = 38300.0 nM 4.42
CHEMBL206604 IC50 = 8200.0 nM -
CHEMBL537947 IC50 > 100000.0 nM -
CHEMBL560436 IC50 > 100000.0 nM -
CHEMBL204656 ELVITEGRAVIR IC50 = 7200.0 nM -