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Assay Detail

CHEMBL888081

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Binding
Inhibition of HIV1 integrase 3'-end processing activity
82
Total Activities
81
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

Discovery of structurally diverse HIV-1 integrase inhibitors based on a chalcone pharmacophore.
Deng J, Sanchez T, Al-Mawsawi LQ, Dayam R, Yunes RA, Garofalo A, Bolger MB, Neamati N.
Bioorg Med Chem (2007) 15 : 4985 -5002
PubMed 17502148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 82 4.42 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240506 1 5.72
CHEMBL388276 1 5.70
CHEMBL241597 1 5.48
CHEMBL239057 1 5.22
CHEMBL241397 1 5.16
CHEMBL401049 1 4.80
CHEMBL241359 1 4.75
CHEMBL239485 1 4.75
CHEMBL240547 1 4.72
CHEMBL401050 1 4.55
CHEMBL394650 1 4.54
CHEMBL391519 1 4.54
CHEMBL239696 1 4.50
CHEMBL239482 1 4.44
CHEMBL392160 1 4.43
CHEMBL240299 1 4.39
CHEMBL240329 1 4.38
CHEMBL241804 1 4.31
CHEMBL148472 1 4.28
CHEMBL395448 1 4.28
CHEMBL241596 1 4.27
CHEMBL240546 1 4.19
CHEMBL239244 1 4.19
CHEMBL241396 1 4.19
CHEMBL241606 1 4.17
CHEMBL391411 1 4.16
CHEMBL239483 1 4.13
CHEMBL239274 1 4.11
CHEMBL391423 1 4.10
CHEMBL240513 1 4.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240506 IC50 = 1900.0 nM 5.72
CHEMBL388276 IC50 = 2000.0 nM 5.70
CHEMBL241597 IC50 = 3300.0 nM 5.48
CHEMBL239057 IC50 = 6000.0 nM 5.22
CHEMBL241397 IC50 = 7000.0 nM 5.16
CHEMBL401049 IC50 = 16000.0 nM 4.80
CHEMBL239485 IC50 = 18000.0 nM 4.75
CHEMBL241359 IC50 = 18000.0 nM 4.75
CHEMBL240547 IC50 = 19000.0 nM 4.72
CHEMBL401050 IC50 = 28000.0 nM 4.55
CHEMBL391519 IC50 = 29000.0 nM 4.54
CHEMBL394650 IC50 = 29000.0 nM 4.54
CHEMBL239696 IC50 = 32000.0 nM 4.50
CHEMBL239482 IC50 = 36000.0 nM 4.44
CHEMBL392160 IC50 = 37000.0 nM 4.43
CHEMBL240299 IC50 = 41000.0 nM 4.39
CHEMBL240329 IC50 = 42000.0 nM 4.38
CHEMBL241804 IC50 = 49000.0 nM 4.31
CHEMBL395448 IC50 = 52000.0 nM 4.28
CHEMBL148472 IC50 = 53000.0 nM 4.28
CHEMBL241596 IC50 = 54000.0 nM 4.27
CHEMBL239244 IC50 = 64000.0 nM 4.19
CHEMBL241396 IC50 = 65000.0 nM 4.19
CHEMBL240546 IC50 = 64000.0 nM 4.19
CHEMBL241606 IC50 = 67000.0 nM 4.17
CHEMBL391411 IC50 = 70000.0 nM 4.16
CHEMBL239483 IC50 = 74000.0 nM 4.13
CHEMBL239274 IC50 = 78000.0 nM 4.11
CHEMBL391423 IC50 = 80000.0 nM 4.10
CHEMBL240513 IC50 = 81000.0 nM 4.09
CHEMBL240511 IC50 = 84000.0 nM 4.08
CHEMBL399006 IC50 = 85000.0 nM 4.07
CHEMBL240331 IC50 = 87000.0 nM 4.06
CHEMBL399412 IC50 = 87000.0 nM 4.06
CHEMBL240752 IC50 = 92000.0 nM 4.04
CHEMBL240543 IC50 = 91000.0 nM 4.04
CHEMBL239484 IC50 = 95000.0 nM 4.02
CHEMBL240974 IC50 = 100000.0 nM 4.00
CHEMBL239056 IC50 = 100000.0 nM 4.00
CHEMBL241598 IC50 = 100000.0 nM 4.00
CHEMBL394458 IC50 > 1000000.0 nM -
CHEMBL240975 IC50 > 100000.0 nM -
CHEMBL391444 IC50 = 679000.0 nM -
CHEMBL240300 IC50 = 857000.0 nM -
CHEMBL241183 IC50 > 100000.0 nM -
CHEMBL238632 IC50 > 100000.0 nM -
CHEMBL241358 IC50 = 212000.0 nM -
CHEMBL240712 IC50 = 161000.0 nM -
CHEMBL238633 IC50 > 100000.0 nM -
CHEMBL227400 IC50 > 100000.0 nM -