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Assay Detail

CHEMBL801709

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Binding
In vitro inhibitory activity against purified recombinant human renin
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Renin (CHEMBL286)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
Vieira E, Binggeli A, Breu V, Bur D, Fischli W, Güller R, Hirth G, Märki HP, Müller M, Oefner C, Scalone M, Stadler H, Wilhelm M, Wostl W.
Bioorg Med Chem Lett (1999) 9 : 1397 -1402
PubMed 10360744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.90 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31601 REMIKIREN 2.0 1 10.60
CHEMBL430539 1 10.22
CHEMBL417485 1 8.82
CHEMBL31466 1 8.10
CHEMBL285454 1 7.58
CHEMBL431502 1 7.39
CHEMBL283683 1 7.28
CHEMBL31252 1 7.26
CHEMBL289898 1 7.06
CHEMBL31886 1 7.04
CHEMBL418034 1 7.00
CHEMBL31587 1 6.80
CHEMBL418031 1 6.80
CHEMBL286580 1 6.68
CHEMBL30755 1 6.66
CHEMBL287637 1 6.66
CHEMBL287139 1 6.27
CHEMBL283237 1 6.24
CHEMBL440654 1 6.13
CHEMBL442264 1 6.06
CHEMBL431689 1 5.58
CHEMBL31479 1 4.58
CHEMBL286733 1 4.40
CHEMBL413256 1 4.30
CHEMBL31997 1 -
CHEMBL417673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31601 REMIKIREN IC50 = 0.025 nM 10.60
CHEMBL430539 IC50 = 0.06 nM 10.22
CHEMBL417485 IC50 = 1.5 nM 8.82
CHEMBL31466 IC50 = 8.0 nM 8.10
CHEMBL285454 IC50 = 26.0 nM 7.58
CHEMBL431502 IC50 = 41.0 nM 7.39
CHEMBL283683 IC50 = 53.0 nM 7.28
CHEMBL31252 IC50 = 55.0 nM 7.26
CHEMBL289898 IC50 = 87.0 nM 7.06
CHEMBL31886 IC50 = 91.0 nM 7.04
CHEMBL418034 IC50 = 100.0 nM 7.00
CHEMBL31587 IC50 = 160.0 nM 6.80
CHEMBL418031 IC50 = 160.0 nM 6.80
CHEMBL286580 IC50 = 210.0 nM 6.68
CHEMBL30755 IC50 = 220.0 nM 6.66
CHEMBL287637 IC50 = 220.0 nM 6.66
CHEMBL287139 IC50 = 540.0 nM 6.27
CHEMBL283237 IC50 = 580.0 nM 6.24
CHEMBL440654 IC50 = 740.0 nM 6.13
CHEMBL442264 IC50 = 880.0 nM 6.06
CHEMBL431689 IC50 = 2600.0 nM 5.58
CHEMBL31479 IC50 = 26000.0 nM 4.58
CHEMBL286733 IC50 = 40000.0 nM 4.40
CHEMBL413256 IC50 = 50000.0 nM 4.30
CHEMBL31997 IC50 = 1200000.0 nM -
CHEMBL417673 IC50 > 1000000.0 nM -