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Assay Detail

CHEMBL4725928

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

Functional
Antiviral activity against HIV1 harboring G140S/Q148H double mutant in presence of 10% FBS
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.
Patel M,Naidu BN,Dicker I,Higley H,Lin Z,Terry B,Protack T,Krystal M,Jenkins S,Parker D,Panja C,Rampulla R,Mathur A,Meanwell NA,Walker MA
Bioorg Med Chem (2020) 28 : 115541 -115541
PubMed 32389483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.48 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4795180 1 8.85
CHEMBL4786078 1 8.52
CHEMBL4744182 1 8.30
CHEMBL4745479 1 8.22
CHEMBL4750708 1 8.10
CHEMBL4745227 1 8.10
CHEMBL4786799 1 8.10
CHEMBL4779601 1 8.00
CHEMBL4760026 1 7.92
CHEMBL4745638 1 7.85
CHEMBL4748499 1 7.77
CHEMBL4788865 1 7.50
CHEMBL4751455 1 7.43
CHEMBL4759219 1 7.41
CHEMBL4782946 1 7.03
CHEMBL4750254 1 6.89
CHEMBL4782667 1 6.44
CHEMBL4755951 1 6.44
CHEMBL4740178 1 6.25
CHEMBL4786092 1 6.15
CHEMBL4760280 1 5.88
CHEMBL4745112 1 -
CHEMBL4750918 1 -
CHEMBL4754986 1 -
CHEMBL4786541 1 -
CHEMBL4760806 1 -
CHEMBL4754233 1 -
CHEMBL4762216 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4795180 EC50 = 1.4 nM 8.85
CHEMBL4786078 EC50 = 3.0 nM 8.52
CHEMBL4744182 EC50 = 5.0 nM 8.30
CHEMBL4745479 EC50 = 6.0 nM 8.22
CHEMBL4750708 EC50 = 8.0 nM 8.10
CHEMBL4745227 EC50 = 8.0 nM 8.10
CHEMBL4786799 EC50 = 8.0 nM 8.10
CHEMBL4779601 EC50 = 10.0 nM 8.00
CHEMBL4760026 EC50 = 12.0 nM 7.92
CHEMBL4745638 EC50 = 14.0 nM 7.85
CHEMBL4748499 EC50 = 17.0 nM 7.77
CHEMBL4788865 EC50 = 32.0 nM 7.50
CHEMBL4751455 EC50 = 37.0 nM 7.43
CHEMBL4759219 EC50 = 39.0 nM 7.41
CHEMBL4782946 EC50 = 94.0 nM 7.03
CHEMBL4750254 EC50 = 129.0 nM 6.89
CHEMBL4782667 EC50 = 361.0 nM 6.44
CHEMBL4755951 EC50 = 363.0 nM 6.44
CHEMBL4740178 EC50 = 558.0 nM 6.25
CHEMBL4786092 EC50 = 714.0 nM 6.15
CHEMBL4760280 EC50 = 1325.0 nM 5.88
CHEMBL4745112 EC50 > 8000.0 nM -
CHEMBL4750918 EC50 > 8000.0 nM -
CHEMBL4754986 EC50 > 8000.0 nM -
CHEMBL4786541 EC50 > 8000.0 nM -
CHEMBL4760806 EC50 > 8000.0 nM -
CHEMBL4754233 EC50 > 8000.0 nM -
CHEMBL4762216 EC50 > 8000.0 nM -