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Assay Detail

CHEMBL803424

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

Binding
Inhibitory activity against purified recombinant human renin
20
Total Activities
20
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

Piperidine-renin inhibitors compounds with improved physicochemical properties.
Güller R, Binggeli A, Breu V, Bur D, Fischli W, Hirth G, Jenny C, Kansy M, Montavon F, Müller M, Oefner C, Stadler H, Vieira E, Wilhelm M, Wostl W, Märki HP.
Bioorg Med Chem Lett (1999) 9 : 1403 -1408
PubMed 10360745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.30 10.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430539 1 10.06
CHEMBL286413 1 9.40
CHEMBL285146 1 9.30
CHEMBL32002 1 9.17
CHEMBL31881 1 9.04
CHEMBL287023 1 8.74
CHEMBL31880 1 8.64
CHEMBL31675 1 8.48
CHEMBL30618 1 8.40
CHEMBL31466 1 8.30
CHEMBL283046 1 8.29
CHEMBL281299 1 8.19
CHEMBL285046 1 8.10
CHEMBL31428 1 8.05
CHEMBL31404 1 8.00
CHEMBL285779 1 7.92
CHEMBL265984 1 7.92
CHEMBL284690 1 7.66
CHEMBL30846 1 6.23
CHEMBL277738 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430539 IC50 = 0.087 nM 10.06
CHEMBL286413 IC50 = 0.4 nM 9.40
CHEMBL285146 IC50 = 0.5 nM 9.30
CHEMBL32002 IC50 = 0.67 nM 9.17
CHEMBL31881 IC50 = 0.92 nM 9.04
CHEMBL287023 IC50 = 1.8 nM 8.74
CHEMBL31880 IC50 = 2.3 nM 8.64
CHEMBL31675 IC50 = 3.3 nM 8.48
CHEMBL30618 IC50 = 4.0 nM 8.40
CHEMBL31466 IC50 = 5.0 nM 8.30
CHEMBL283046 IC50 = 5.1 nM 8.29
CHEMBL281299 IC50 = 6.4 nM 8.19
CHEMBL285046 IC50 = 8.0 nM 8.10
CHEMBL31428 IC50 = 9.0 nM 8.05
CHEMBL31404 IC50 = 10.0 nM 8.00
CHEMBL285779 IC50 = 12.0 nM 7.92
CHEMBL265984 IC50 = 12.0 nM 7.92
CHEMBL284690 IC50 = 22.0 nM 7.66
CHEMBL30846 IC50 = 590.0 nM 6.23
CHEMBL277738 IC50 = 820.0 nM 6.09