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Assay Detail

CHEMBL763310

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

Binding
Inhibition of HIV-1 protease.
20
Total Activities
20
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

Synthesis and pharmacological evaluation of sulfone substituted HIV protease inhibitors
Schwartz TM, Bundy GL, Strohbach JW, Thaisrivongs S, Johnson PD, Skulnick HI, Tomich PK, Lynn JC, Chong KT, Hinshaw RR, Raub TJ, Padbury GE, Toth LN
Bioorg Med Chem Lett (1997) 7 : 399 -402
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.55 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130184 1 9.18
CHEMBL128629 1 9.14
CHEMBL2062136 1 9.10
CHEMBL16636 1 9.07
CHEMBL132275 1 8.96
CHEMBL131128 1 8.72
CHEMBL129802 1 8.72
CHEMBL131064 1 8.68
CHEMBL127219 1 8.64
CHEMBL338756 1 8.52
CHEMBL16400 1 8.52
CHEMBL279580 1 8.52
CHEMBL277309 1 8.51
CHEMBL340638 1 8.51
CHEMBL131395 1 8.39
CHEMBL131658 1 8.22
CHEMBL131317 1 8.15
CHEMBL16711 1 7.96
CHEMBL80882 1 7.80
CHEMBL131821 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130184 Ki = 0.66 nM 9.18
CHEMBL128629 Ki = 0.73 nM 9.14
CHEMBL2062136 Ki = 0.8 nM 9.10
CHEMBL16636 Ki = 0.86 nM 9.07
CHEMBL132275 Ki = 1.1 nM 8.96
CHEMBL131128 Ki = 1.9 nM 8.72
CHEMBL129802 Ki = 1.9 nM 8.72
CHEMBL131064 Ki = 2.1 nM 8.68
CHEMBL127219 Ki = 2.3 nM 8.64
CHEMBL338756 Ki = 3.0 nM 8.52
CHEMBL16400 Ki = 3.0 nM 8.52
CHEMBL279580 Ki = 3.0 nM 8.52
CHEMBL277309 Ki = 3.1 nM 8.51
CHEMBL340638 Ki = 3.1 nM 8.51
CHEMBL131395 Ki = 4.1 nM 8.39
CHEMBL131658 Ki = 6.0 nM 8.22
CHEMBL131317 Ki = 7.0 nM 8.15
CHEMBL16711 Ki = 11.0 nM 7.96
CHEMBL80882 Ki = 16.0 nM 7.80
CHEMBL131821 Ki = 19.0 nM 7.72