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Assay Detail

CHEMBL763391

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Binding
Inhibition of HIV protease, measured by assaying the cleavage of a fluorescent peptide substrate using HPLC
26
Total Activities
26
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 Expert

Target

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Han Q, Chang CH, Li R, Ru Y, Jadhav PK, Lam PY.
J Med Chem (1998) 41 : 2019 -2028
PubMed 9622543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 9.83 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305125 1 11.00
CHEMBL431174 1 10.74
CHEMBL61173 1 10.68
CHEMBL38314 1 10.57
CHEMBL292858 1 10.51
CHEMBL303128 1 10.51
CHEMBL60352 1 10.46
CHEMBL292631 1 10.43
CHEMBL293654 1 10.28
CHEMBL304713 1 10.28
CHEMBL289473 1 10.22
CHEMBL64300 1 9.85
CHEMBL434019 1 9.80
CHEMBL294582 1 9.80
CHEMBL60370 1 9.77
CHEMBL444038 1 9.77
CHEMBL291621 1 9.72
CHEMBL291814 1 9.68
CHEMBL292043 1 9.59
CHEMBL223824 MOZENAVIR 2.0 1 9.55
CHEMBL294331 1 9.36
CHEMBL304491 1 9.21
CHEMBL304411 1 8.85
CHEMBL304410 1 8.44
CHEMBL294295 1 8.41
CHEMBL302864 1 8.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305125 Ki = 0.01 nM 11.00
CHEMBL431174 Ki = 0.018 nM 10.74
CHEMBL61173 Ki = 0.021 nM 10.68
CHEMBL38314 Ki = 0.027 nM 10.57
CHEMBL292858 Ki = 0.031 nM 10.51
CHEMBL303128 Ki = 0.031 nM 10.51
CHEMBL60352 Ki = 0.035 nM 10.46
CHEMBL292631 Ki = 0.037 nM 10.43
CHEMBL293654 Ki = 0.052 nM 10.28
CHEMBL304713 Ki = 0.052 nM 10.28
CHEMBL289473 Ki = 0.06 nM 10.22
CHEMBL64300 Ki = 0.14 nM 9.85
CHEMBL434019 Ki = 0.16 nM 9.80
CHEMBL294582 Ki = 0.16 nM 9.80
CHEMBL60370 Ki = 0.17 nM 9.77
CHEMBL444038 Ki = 0.17 nM 9.77
CHEMBL291621 Ki = 0.19 nM 9.72
CHEMBL291814 Ki = 0.21 nM 9.68
CHEMBL292043 Ki = 0.26 nM 9.59
CHEMBL223824 MOZENAVIR Ki = 0.28 nM 9.55
CHEMBL294331 Ki = 0.44 nM 9.36
CHEMBL304491 Ki = 0.62 nM 9.21
CHEMBL304411 Ki = 1.4 nM 8.85
CHEMBL304410 Ki = 3.6 nM 8.44
CHEMBL294295 Ki = 3.9 nM 8.41
CHEMBL302864 Ki = 6.6 nM 8.18