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Assay Detail

CHEMBL801758

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Binding
The concentration producing 50% inhibition of renin activity in monkey plasma was determined by radioimmunoassay.
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.
Doherty AM, Sircar I, Kornberg BE, Quin J, Winters RT, Kaltenbronn JS, Taylor MD, Batley BL, Rapundalo SR, Ryan MJ.
J Med Chem (1992) 35 : 2 -14
PubMed 1732531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 9.02 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286147 1 10.00
CHEMBL31910 1 9.68
CHEMBL286951 1 9.66
CHEMBL29323 1 9.64
CHEMBL281531 1 9.64
CHEMBL21684 1 9.62
CHEMBL28702 1 9.60
CHEMBL32575 1 9.55
CHEMBL29103 1 9.52
CHEMBL31259 1 9.51
CHEMBL282756 1 9.49
CHEMBL285095 1 9.46
CHEMBL31956 1 9.46
CHEMBL286085 1 9.44
CHEMBL31679 1 9.40
CHEMBL405764 1 9.38
CHEMBL284254 1 9.36
CHEMBL28408 1 9.34
CHEMBL405227 1 9.30
CHEMBL31420 1 9.24
CHEMBL285207 1 9.21
CHEMBL31889 1 9.16
CHEMBL31550 1 9.15
CHEMBL31621 1 9.10
CHEMBL30920 1 9.09
CHEMBL1790136 1 9.09
CHEMBL265316 1 9.06
CHEMBL262107 1 9.05
CHEMBL31268 1 9.04
CHEMBL280818 1 8.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286147 IC50 = 0.1 nM 10.00
CHEMBL31910 IC50 = 0.21 nM 9.68
CHEMBL286951 IC50 = 0.22 nM 9.66
CHEMBL29323 IC50 = 0.23 nM 9.64
CHEMBL281531 IC50 = 0.23 nM 9.64
CHEMBL21684 IC50 = 0.24 nM 9.62
CHEMBL28702 IC50 = 0.25 nM 9.60
CHEMBL32575 IC50 = 0.28 nM 9.55
CHEMBL29103 IC50 = 0.3 nM 9.52
CHEMBL31259 IC50 = 0.31 nM 9.51
CHEMBL282756 IC50 = 0.32 nM 9.49
CHEMBL31956 IC50 = 0.35 nM 9.46
CHEMBL285095 IC50 = 0.35 nM 9.46
CHEMBL286085 IC50 = 0.36 nM 9.44
CHEMBL31679 IC50 = 0.4 nM 9.40
CHEMBL405764 IC50 = 0.42 nM 9.38
CHEMBL284254 IC50 = 0.44 nM 9.36
CHEMBL28408 IC50 = 0.46 nM 9.34
CHEMBL405227 IC50 = 0.5 nM 9.30
CHEMBL31420 IC50 = 0.57 nM 9.24
CHEMBL285207 IC50 = 0.62 nM 9.21
CHEMBL31889 IC50 = 0.69 nM 9.16
CHEMBL31550 IC50 = 0.7 nM 9.15
CHEMBL31621 IC50 = 0.79 nM 9.10
CHEMBL30920 IC50 = 0.81 nM 9.09
CHEMBL1790136 IC50 = 0.82 nM 9.09
CHEMBL265316 IC50 = 0.87 nM 9.06
CHEMBL262107 IC50 = 0.9 nM 9.05
CHEMBL31268 IC50 = 0.92 nM 9.04
CHEMBL280818 IC50 = 1.17 nM 8.93
CHEMBL287423 IC50 = 1.2 nM 8.92
CHEMBL32239 IC50 = 1.49 nM 8.83
CHEMBL280543 IC50 = 1.5 nM 8.82
CHEMBL284922 IC50 = 1.89 nM 8.72
CHEMBL28132 IC50 = 2.0 nM 8.70
CHEMBL287265 IC50 = 2.33 nM 8.63
CHEMBL29041 IC50 = 2.46 nM 8.61
CHEMBL28311 IC50 = 2.96 nM 8.53
CHEMBL262385 IC50 = 3.55 nM 8.45
CHEMBL31438 IC50 = 10.0 nM 8.00
CHEMBL31201 IC50 = 12.3 nM 7.91
CHEMBL285778 IC50 = 19.1 nM 7.72
CHEMBL32046 IC50 = 97.8 nM 7.01
CHEMBL285884 IC50 = 164.0 nM 6.79