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Assay Detail

CHEMBL769512

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Binding
Inhibitory activity against HIV-1 protease
ChEMBL ↗
67
Total Activities
67
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: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas.
Lam PY, Ru Y, Jadhav PK, Aldrich PE, DeLucca GV, Eyermann CJ, Chang CH, Emmett G, Holler ER, Daneker WF, Li L, Confalone PN, McHugh RJ, Han Q, Li R, Markwalder JA, Seitz SP, Sharpe TR, Bacheler LT, Rayner MM, Klabe RM, Shum L, Winslow DL, Kornhauser DM, Hodge CN.
J Med Chem (1996) 39 : 3514 -3525
PubMed 8784449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 8.03 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284136 — — 1 9.92
CHEMBL35860 — — 1 9.92
CHEMBL285417 — — 1 9.85
CHEMBL431684 — — 1 9.55
CHEMBL334180 — — 1 9.55
CHEMBL430702 — — 1 9.51
CHEMBL412810 — — 1 9.48
CHEMBL21145 DMP-323 — 1 9.47
CHEMBL85294 — — 1 9.38
CHEMBL85915 — — 1 9.22
CHEMBL312930 — — 1 9.05
CHEMBL87408 — — 1 9.03
CHEMBL87592 — — 1 9.00
CHEMBL313520 — — 1 8.96
CHEMBL287355 — — 1 8.89
CHEMBL284472 — — 1 8.85
CHEMBL315174 — — 1 8.85
CHEMBL85771 — — 1 8.85
CHEMBL313732 — — 1 8.85
CHEMBL86959 — — 1 8.82
CHEMBL313289 — — 1 8.80
CHEMBL420054 — — 1 8.80
CHEMBL286393 — — 1 8.74
CHEMBL431306 — — 1 8.68
CHEMBL87476 — — 1 8.64
CHEMBL415040 — — 1 8.55
CHEMBL418939 — — 1 8.52
CHEMBL290576 — — 1 8.52
CHEMBL315306 — — 1 8.44
CHEMBL287274 — — 1 8.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284136 — Ki = 0.12 nM 9.92
CHEMBL35860 — Ki = 0.12 nM 9.92
CHEMBL285417 — Ki = 0.14 nM 9.85
CHEMBL431684 — Ki = 0.28 nM 9.55
CHEMBL334180 — Ki = 0.28 nM 9.55
CHEMBL430702 — Ki = 0.31 nM 9.51
CHEMBL412810 — Ki = 0.33 nM 9.48
CHEMBL21145 DMP-323 Ki = 0.34 nM 9.47
CHEMBL85294 — Ki = 0.42 nM 9.38
CHEMBL85915 — Ki = 0.6 nM 9.22
CHEMBL312930 — Ki = 0.89 nM 9.05
CHEMBL87408 — Ki = 0.93 nM 9.03
CHEMBL87592 — Ki = 1.0 nM 9.00
CHEMBL313520 — Ki = 1.1 nM 8.96
CHEMBL287355 — Ki = 1.3 nM 8.89
CHEMBL284472 — Ki = 1.4 nM 8.85
CHEMBL313732 — Ki = 1.4 nM 8.85
CHEMBL85771 — Ki = 1.4 nM 8.85
CHEMBL315174 — Ki = 1.4 nM 8.85
CHEMBL86959 — Ki = 1.5 nM 8.82
CHEMBL313289 — Ki = 1.6 nM 8.80
CHEMBL420054 — Ki = 1.6 nM 8.80
CHEMBL286393 — Ki = 1.8 nM 8.74
CHEMBL431306 — Ki = 2.1 nM 8.68
CHEMBL87476 — Ki = 2.3 nM 8.64
CHEMBL415040 — Ki = 2.8 nM 8.55
CHEMBL290576 — Ki = 3.0 nM 8.52
CHEMBL418939 — Ki = 3.0 nM 8.52
CHEMBL315306 — Ki = 3.6 nM 8.44
CHEMBL287274 — Ki = 4.3 nM 8.37
CHEMBL314052 — Ki = 4.6 nM 8.34
CHEMBL87991 — Ki = 5.2 nM 8.28
CHEMBL314709 — Ki = 5.2 nM 8.28
CHEMBL284314 — Ki = 5.2 nM 8.28
CHEMBL422772 — Ki = 5.7 nM 8.24
CHEMBL315300 — Ki = 6.9 nM 8.16
CHEMBL314984 — Ki = 7.0 nM 8.15
CHEMBL84734 — Ki = 7.0 nM 8.15
CHEMBL313188 — Ki = 7.3 nM 8.14
CHEMBL32733 — Ki = 8.0 nM 8.10
CHEMBL315639 — Ki = 9.7 nM 8.01
CHEMBL284491 — Ki = 12.0 nM 7.92
CHEMBL314944 — Ki = 22.0 nM 7.66
CHEMBL313008 — Ki = 22.0 nM 7.66
CHEMBL87919 — Ki = 27.0 nM 7.57
CHEMBL316256 — Ki = 30.0 nM 7.52
CHEMBL87142 — Ki = 34.0 nM 7.47
CHEMBL432993 — Ki = 36.0 nM 7.44
CHEMBL32828 — Ki = 37.0 nM 7.43
CHEMBL86874 — Ki = 49.0 nM 7.31