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Assay Detail

CHEMBL801744

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

Binding
In vitro inhibition of monkey renin.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Patt WC, Hamilton HW, Taylor MD, Ryan MJ, Taylor DG, Connolly CJ, Doherty AM, Klutchko SR, Sircar I, Steinbaugh BA.
J Med Chem (1992) 35 : 2562 -2572
PubMed 1635057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 9.03 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88091 1 9.80
CHEMBL313063 1 9.70
CHEMBL315380 1 9.64
CHEMBL88069 1 9.57
CHEMBL315211 1 9.55
CHEMBL316208 1 9.46
CHEMBL34894 1 9.44
CHEMBL263531 1 9.32
CHEMBL405227 1 9.30
CHEMBL431217 1 9.27
CHEMBL314066 1 9.24
CHEMBL430634 1 9.23
CHEMBL300337 ENALKIREN 2.0 1 9.12
CHEMBL293196 1 9.08
CHEMBL85672 1 9.04
CHEMBL420417 1 8.63
CHEMBL60610 1 8.57
CHEMBL315992 1 8.47
CHEMBL316218 1 8.44
CHEMBL87389 1 8.39
CHEMBL316176 1 7.86
CHEMBL86374 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88091 IC50 = 0.16 nM 9.80
CHEMBL313063 IC50 = 0.2 nM 9.70
CHEMBL315380 IC50 = 0.23 nM 9.64
CHEMBL88069 IC50 = 0.27 nM 9.57
CHEMBL315211 IC50 = 0.28 nM 9.55
CHEMBL316208 IC50 = 0.35 nM 9.46
CHEMBL34894 IC50 = 0.36 nM 9.44
CHEMBL263531 IC50 = 0.48 nM 9.32
CHEMBL405227 IC50 = 0.5 nM 9.30
CHEMBL431217 IC50 = 0.54 nM 9.27
CHEMBL314066 IC50 = 0.581 nM 9.24
CHEMBL430634 IC50 = 0.59 nM 9.23
CHEMBL300337 ENALKIREN IC50 = 0.76 nM 9.12
CHEMBL293196 IC50 = 0.83 nM 9.08
CHEMBL85672 IC50 = 0.91 nM 9.04
CHEMBL420417 IC50 = 2.34 nM 8.63
CHEMBL60610 IC50 = 2.7 nM 8.57
CHEMBL315992 IC50 = 3.4 nM 8.47
CHEMBL316218 IC50 = 3.61 nM 8.44
CHEMBL87389 IC50 = 4.1 nM 8.39
CHEMBL316176 IC50 = 13.7 nM 7.86
CHEMBL86374 IC50 = 33.0 nM 7.48