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Assay Detail

CHEMBL1049070

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Binding
Inhibition of HIV1 protease expressed in Escherichia coli K12 assessed as inhibition of enzyme activity
31
Total Activities
31
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

Protease (CHEMBL2366517)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

3D-QSAR CoMFA/CoMSIA models based on theoretical active conformers of HOE/BAY-793 analogs derived from HIV-1 protease inhibitor complexes.
da Cunha EF, Sippl W, de Castro Ramalho T, Ceva Antunes OA, de Alencastro RB, Albuquerque MG.
Eur J Med Chem (2009) 44 : 4344 -4352
PubMed 19616874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.55 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL568589 1 9.52
CHEMBL566620 1 9.52
CHEMBL569671 1 9.52
CHEMBL568883 1 9.52
CHEMBL568951 1 9.47
CHEMBL565964 1 9.40
CHEMBL566849 1 9.40
CHEMBL566842 1 9.30
CHEMBL566902 1 9.13
CHEMBL568840 1 9.10
CHEMBL568832 1 9.10
CHEMBL567444 1 9.07
CHEMBL565528 1 9.05
CHEMBL569670 1 9.00
CHEMBL569236 1 8.89
CHEMBL569569 1 8.85
CHEMBL568365 1 8.77
CHEMBL289846 1 8.70
CHEMBL571731 1 8.66
CHEMBL567043 1 8.54
CHEMBL569673 1 8.49
CHEMBL568977 1 8.40
CHEMBL568817 1 8.40
CHEMBL406493 A-76928 1 7.82
CHEMBL566839 1 7.74
CHEMBL570827 1 7.66
CHEMBL569111 1 7.42
CHEMBL567500 1 7.00
CHEMBL565766 1 6.85
CHEMBL569672 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL568589 IC50 = 0.302 nM 9.52
CHEMBL566620 IC50 = 0.302 nM 9.52
CHEMBL569671 IC50 = 0.302 nM 9.52
CHEMBL568883 IC50 = 0.302 nM 9.52
CHEMBL568951 IC50 = 0.3388 nM 9.47
CHEMBL565964 IC50 = 0.3981 nM 9.40
CHEMBL566849 IC50 = 0.3981 nM 9.40
CHEMBL566842 IC50 = 0.5012 nM 9.30
CHEMBL566902 IC50 = 0.7413 nM 9.13
CHEMBL568840 IC50 = 0.7943 nM 9.10
CHEMBL568832 IC50 = 0.7943 nM 9.10
CHEMBL567444 IC50 = 0.8511 nM 9.07
CHEMBL565528 IC50 = 0.8913 nM 9.05
CHEMBL569670 IC50 = 1.0 nM 9.00
CHEMBL569236 IC50 = 1.288 nM 8.89
CHEMBL569569 IC50 = 1.413 nM 8.85
CHEMBL568365 IC50 = 1.698 nM 8.77
CHEMBL289846 IC50 = 1.995 nM 8.70
CHEMBL571731 IC50 = 2.188 nM 8.66
CHEMBL567043 IC50 = 2.884 nM 8.54
CHEMBL569673 IC50 = 3.236 nM 8.49
CHEMBL568977 IC50 = 3.981 nM 8.40
CHEMBL568817 IC50 = 3.981 nM 8.40
CHEMBL406493 A-76928 IC50 = 15.14 nM 7.82
CHEMBL566839 IC50 = 18.2 nM 7.74
CHEMBL570827 IC50 = 21.88 nM 7.66
CHEMBL569111 IC50 = 38.02 nM 7.42
CHEMBL567500 IC50 = 100.0 nM 7.00
CHEMBL565766 IC50 = 141.25 nM 6.85
CHEMBL569672 IC50 = 338.84 nM 6.47
CHEMBL569573 IC50 = 363.08 nM 6.44