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Assay Detail

CHEMBL1033787

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

Functional
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
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
EC50 52 5.97 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203443 1 7.70
CHEMBL549549 1 7.22
CHEMBL379664 1 7.10
CHEMBL550893 1 7.00
CHEMBL549546 1 6.89
CHEMBL549611 1 6.75
CHEMBL561099 1 6.54
CHEMBL562360 1 6.48
CHEMBL550895 1 6.47
CHEMBL242883 1 6.36
CHEMBL550691 1 6.35
CHEMBL558286 1 6.33
CHEMBL559903 1 6.29
CHEMBL560439 1 6.28
CHEMBL563162 1 6.27
CHEMBL561437 1 6.24
CHEMBL550220 1 6.22
CHEMBL551437 1 6.19
CHEMBL204656 ELVITEGRAVIR 4.0 1 6.05
CHEMBL565125 1 5.89
CHEMBL550080 1 5.89
CHEMBL558287 1 5.78
CHEMBL549750 1 5.70
CHEMBL551235 1 5.69
CHEMBL561827 1 5.63
CHEMBL560836 1 5.55
CHEMBL560234 1 5.47
CHEMBL561619 1 5.14
CHEMBL206604 1 5.12
CHEMBL563677 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203443 EC50 = 20.0 nM 7.70
CHEMBL549549 EC50 = 60.0 nM 7.22
CHEMBL379664 EC50 = 80.0 nM 7.10
CHEMBL550893 EC50 = 100.0 nM 7.00
CHEMBL549546 EC50 = 130.0 nM 6.89
CHEMBL549611 EC50 = 180.0 nM 6.75
CHEMBL561099 EC50 = 290.0 nM 6.54
CHEMBL562360 EC50 = 330.0 nM 6.48
CHEMBL550895 EC50 = 340.0 nM 6.47
CHEMBL242883 EC50 = 440.0 nM 6.36
CHEMBL550691 EC50 = 450.0 nM 6.35
CHEMBL558286 EC50 = 470.0 nM 6.33
CHEMBL559903 EC50 = 510.0 nM 6.29
CHEMBL560439 EC50 = 530.0 nM 6.28
CHEMBL563162 EC50 = 540.0 nM 6.27
CHEMBL561437 EC50 = 570.0 nM 6.24
CHEMBL550220 EC50 = 600.0 nM 6.22
CHEMBL551437 EC50 = 640.0 nM 6.19
CHEMBL204656 ELVITEGRAVIR EC50 = 900.0 nM 6.05
CHEMBL565125 EC50 = 1300.0 nM 5.89
CHEMBL550080 EC50 = 1300.0 nM 5.89
CHEMBL558287 EC50 = 1680.0 nM 5.78
CHEMBL549750 EC50 = 2000.0 nM 5.70
CHEMBL551235 EC50 = 2040.0 nM 5.69
CHEMBL561827 EC50 = 2340.0 nM 5.63
CHEMBL560836 EC50 = 2800.0 nM 5.55
CHEMBL560234 EC50 = 3400.0 nM 5.47
CHEMBL561619 EC50 = 7300.0 nM 5.14
CHEMBL206604 EC50 = 7500.0 nM 5.12
CHEMBL563677 EC50 = 9800.0 nM 5.01
CHEMBL558481 EC50 = 13590.0 nM 4.87
CHEMBL561423 EC50 = 15900.0 nM 4.80
CHEMBL549816 EC50 = 17100.0 nM 4.77
CHEMBL563525 EC50 = 27700.0 nM 4.56
CHEMBL557891 EC50 = 51600.0 nM 4.29
CHEMBL560960 EC50 > 6000.0 nM -
CHEMBL537947 EC50 > 6000.0 nM -
CHEMBL561100 EC50 > 30000.0 nM -
CHEMBL554722 EC50 = 115500.0 nM -
CHEMBL549404 EC50 > 6000.0 nM -
CHEMBL549338 EC50 > 6000.0 nM -
CHEMBL560761 EC50 > 6000.0 nM -
CHEMBL560436 EC50 > 30000.0 nM -
CHEMBL549405 EC50 > 6000.0 nM -
CHEMBL381059 EC50 > 30000.0 nM -
CHEMBL557480 EC50 > 30000.0 nM -
CHEMBL408699 EC50 = 108800.0 nM -
CHEMBL382680 EC50 > 30000.0 nM -
CHEMBL560235 EC50 > 30000.0 nM -
CHEMBL559705 EC50 > 6000.0 nM -