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Assay Detail

CHEMBL671393

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Binding
Binding affinity to Endothelin B receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of IRL 3461: a novel and potent endothelin antagonist with balanced ETA/ETB affinity.
Sakaki J, Murata T, Yuumoto Y, Nakamura I, Trueh T, Pitterna T, Iwasaki G, Oda K, Yamamura T, Hayakawa K.
Bioorg Med Chem Lett (1998) 8 : 2241 -2246
PubMed 9873521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 9.15 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310039 1 9.85
CHEMBL433106 1 9.68
CHEMBL305462 1 9.64
CHEMBL72924 1 9.64
CHEMBL308102 1 9.64
CHEMBL306950 1 9.62
CHEMBL72348 1 9.62
CHEMBL310920 1 9.47
CHEMBL73373 1 9.42
CHEMBL73000 1 9.42
CHEMBL307471 1 9.41
CHEMBL307045 1 9.31
CHEMBL308269 1 9.30
CHEMBL307384 1 9.23
CHEMBL307470 1 9.22
CHEMBL73835 1 9.15
CHEMBL70686 1 9.12
CHEMBL73697 1 9.10
CHEMBL72410 1 9.00
CHEMBL311854 1 8.92
CHEMBL72217 1 8.89
CHEMBL72358 1 8.51
CHEMBL263301 1 8.49
CHEMBL73042 1 8.46
CHEMBL70310 1 8.36
CHEMBL439759 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310039 Ki = 0.14 nM 9.85
CHEMBL433106 Ki = 0.21 nM 9.68
CHEMBL305462 Ki = 0.23 nM 9.64
CHEMBL72924 Ki = 0.23 nM 9.64
CHEMBL308102 Ki = 0.23 nM 9.64
CHEMBL306950 Ki = 0.24 nM 9.62
CHEMBL72348 Ki = 0.24 nM 9.62
CHEMBL310920 Ki = 0.34 nM 9.47
CHEMBL73373 Ki = 0.38 nM 9.42
CHEMBL73000 Ki = 0.38 nM 9.42
CHEMBL307471 Ki = 0.39 nM 9.41
CHEMBL307045 Ki = 0.49 nM 9.31
CHEMBL308269 Ki = 0.5 nM 9.30
CHEMBL307384 Ki = 0.59 nM 9.23
CHEMBL307470 Ki = 0.6 nM 9.22
CHEMBL73835 Ki = 0.7 nM 9.15
CHEMBL70686 Ki = 0.76 nM 9.12
CHEMBL73697 Ki = 0.79 nM 9.10
CHEMBL72410 Ki = 1.0 nM 9.00
CHEMBL311854 Ki = 1.2 nM 8.92
CHEMBL72217 Ki = 1.3 nM 8.89
CHEMBL72358 Ki = 3.1 nM 8.51
CHEMBL263301 Ki = 3.2 nM 8.49
CHEMBL73042 Ki = 3.5 nM 8.46
CHEMBL70310 Ki = 4.4 nM 8.36
CHEMBL439759 Ki = 36.0 nM 7.44