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Assay Detail

CHEMBL682364

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

Binding
Inhibitory activity against [125I]ET1 binding to human endothelin A receptor
ChEMBL ↗
25
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL252) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of a novel class of endothelin receptor selective antagonists; 6-carboxy-2-isopropylamino-5,7-diarylcyclopenteno[1,2-b]pyridines.
Takahashi H, Ohtake N, Sakamoto T, Iino T, Kawanishi N, Nakamura M, Yoshizumi T, Niiyama K, Ozaki S, Okada H, Kano A, Takahashi H, Ishii Y, Okada M, Saito M, Sawazaki Y, Hayama T, Nishikibe M.
Bioorg Med Chem Lett (2004) 14 : 1503 -1507
PubMed 15006391 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 10.26 10.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL289634 — — 2 10.96
CHEMBL286621 — — 2 10.96
CHEMBL411925 — — 2 10.96
CHEMBL287683 — — 2 10.85
CHEMBL432856 — — 1 10.85
CHEMBL35984 — — 1 10.66
CHEMBL37427 — — 1 10.57
CHEMBL287622 — — 1 10.51
CHEMBL289216 — — 2 10.44
CHEMBL288247 — — 2 10.39
CHEMBL36627 — — 1 10.33
CHEMBL287711 — — 1 10.21
CHEMBL37920 — — 1 10.19
CHEMBL290181 — — 1 9.96
CHEMBL36671 — — 1 9.66
CHEMBL291247 — — 1 9.39
CHEMBL38000 — — 1 9.13
CHEMBL287517 — — 1 9.10
CHEMBL37973 — — 1 9.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL289634 — IC50 = 0.011 nM 10.96
CHEMBL286621 — IC50 = 0.011 nM 10.96
CHEMBL411925 — IC50 = 0.011 nM 10.96
CHEMBL287683 — IC50 = 0.014 nM 10.85
CHEMBL432856 — IC50 = 0.014 nM 10.85
CHEMBL35984 — IC50 = 0.022 nM 10.66
CHEMBL287683 — IC50 = 0.024 nM 10.62
CHEMBL289634 — IC50 = 0.025 nM 10.60
CHEMBL37427 — IC50 = 0.027 nM 10.57
CHEMBL287622 — IC50 = 0.031 nM 10.51
CHEMBL289216 — IC50 = 0.036 nM 10.44
CHEMBL288247 — IC50 = 0.041 nM 10.39
CHEMBL411925 — IC50 = 0.045 nM 10.35
CHEMBL36627 — IC50 = 0.047 nM 10.33
CHEMBL286621 — IC50 = 0.048 nM 10.32
CHEMBL289216 — IC50 = 0.057 nM 10.24
CHEMBL288247 — IC50 = 0.059 nM 10.23
CHEMBL287711 — IC50 = 0.062 nM 10.21
CHEMBL37920 — IC50 = 0.065 nM 10.19
CHEMBL290181 — IC50 = 0.11 nM 9.96
CHEMBL36671 — IC50 = 0.22 nM 9.66
CHEMBL291247 — IC50 = 0.41 nM 9.39
CHEMBL38000 — IC50 = 0.74 nM 9.13
CHEMBL287517 — IC50 = 0.8 nM 9.10
CHEMBL37973 — IC50 = 0.86 nM 9.07