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Assay Detail

CHEMBL659791

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Binding
Compound was evaluated for inhibitory activity against human heart chymase (HHC)
27
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

Chymase (CHEMBL4068)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.
Eda M, Ashimori A, Akahoshi F, Yoshimura T, Inoue Y, Fukaya C, Nakajima M, Fukuyama H, Imada T, Takai S, Shiota N, Miyazaki M, Nakamura N.
Bioorg Med Chem Lett (1998) 8 : 913 -918
PubMed 9871511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.41 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353816 1 8.89
CHEMBL170200 1 8.51
CHEMBL287318 1 8.25
CHEMBL170878 1 8.20
CHEMBL170718 1 8.19
CHEMBL170879 1 8.17
CHEMBL170838 1 8.15
CHEMBL170074 2 8.13
CHEMBL172873 1 7.90
CHEMBL171676 1 7.88
CHEMBL352917 1 7.79
CHEMBL171801 1 7.78
CHEMBL171119 1 7.74
CHEMBL173989 1 7.62
CHEMBL170683 1 7.54
CHEMBL369796 1 7.52
CHEMBL170402 1 7.44
CHEMBL147013 1 7.25
CHEMBL171805 1 7.18
CHEMBL171492 1 7.15
CHEMBL368262 1 6.31
CHEMBL171354 1 6.29
CHEMBL172849 1 6.00
CHEMBL368502 1 5.98
CHEMBL355609 1 5.81
CHEMBL172078 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353816 Ki = 1.3 nM 8.89
CHEMBL170200 Ki = 3.1 nM 8.51
CHEMBL287318 Ki = 5.6 nM 8.25
CHEMBL170878 Ki = 6.3 nM 8.20
CHEMBL170718 Ki = 6.5 nM 8.19
CHEMBL170879 Ki = 6.8 nM 8.17
CHEMBL170838 Ki = 7.1 nM 8.15
CHEMBL170074 Ki = 7.4 nM 8.13
CHEMBL172873 Ki = 12.5 nM 7.90
CHEMBL171676 Ki = 13.1 nM 7.88
CHEMBL352917 Ki = 16.3 nM 7.79
CHEMBL171801 Ki = 16.5 nM 7.78
CHEMBL171119 Ki = 18.3 nM 7.74
CHEMBL173989 Ki = 24.0 nM 7.62
CHEMBL170683 Ki = 28.7 nM 7.54
CHEMBL369796 Ki = 30.1 nM 7.52
CHEMBL170402 Ki = 36.4 nM 7.44
CHEMBL147013 Ki = 55.8 nM 7.25
CHEMBL171805 Ki = 65.6 nM 7.18
CHEMBL171492 Ki = 70.1 nM 7.15
CHEMBL170074 Ki = 92.4 nM 7.03
CHEMBL368262 Ki = 493.0 nM 6.31
CHEMBL171354 Ki = 513.0 nM 6.29
CHEMBL172849 Ki = 1010.0 nM 6.00
CHEMBL368502 Ki = 1040.0 nM 5.98
CHEMBL355609 Ki = 1550.0 nM 5.81
CHEMBL172078 Ki = 3620.0 nM 5.44