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Assay Detail

CHEMBL677402

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Binding
In vitro binding affinity to endothelin B receptor in rat cerebellum
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin receptor type B (CHEMBL4631)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Zhang J, Didierlaurent S, Fortin M, Lefrançois D, Uridat E, Vevert JP.
Bioorg Med Chem Lett (2000) 10 : 2575 -2578
PubMed 11086733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.62 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313153 1 8.77
CHEMBL87070 1 8.59
CHEMBL313044 1 8.49
CHEMBL314973 1 8.49
CHEMBL315280 1 8.48
CHEMBL314454 1 8.47
CHEMBL86505 1 8.40
CHEMBL87801 1 8.34
CHEMBL314974 1 8.31
CHEMBL314357 1 8.20
CHEMBL314206 1 8.07
CHEMBL312979 1 8.01
CHEMBL316187 1 8.01
CHEMBL88011 1 8.00
CHEMBL315622 1 7.96
CHEMBL315936 1 7.83
CHEMBL313920 1 7.58
CHEMBL315752 1 7.51
CHEMBL26474 1 7.47
CHEMBL312854 1 7.36
CHEMBL315638 1 7.05
CHEMBL315175 1 6.88
CHEMBL315788 1 6.75
CHEMBL88019 1 6.36
CHEMBL315805 1 6.09
CHEMBL86965 1 6.08
CHEMBL86821 1 6.02
CHEMBL315087 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313153 IC50 = 1.7 nM 8.77
CHEMBL87070 IC50 = 2.6 nM 8.59
CHEMBL313044 IC50 = 3.2 nM 8.49
CHEMBL314973 IC50 = 3.2 nM 8.49
CHEMBL315280 IC50 = 3.3 nM 8.48
CHEMBL314454 IC50 = 3.4 nM 8.47
CHEMBL86505 IC50 = 4.0 nM 8.40
CHEMBL87801 IC50 = 4.6 nM 8.34
CHEMBL314974 IC50 = 4.9 nM 8.31
CHEMBL314357 IC50 = 6.3 nM 8.20
CHEMBL314206 IC50 = 8.6 nM 8.07
CHEMBL312979 IC50 = 9.8 nM 8.01
CHEMBL316187 IC50 = 9.7 nM 8.01
CHEMBL88011 IC50 = 9.9 nM 8.00
CHEMBL315622 IC50 = 11.0 nM 7.96
CHEMBL315936 IC50 = 14.8 nM 7.83
CHEMBL313920 IC50 = 26.0 nM 7.58
CHEMBL315752 IC50 = 31.0 nM 7.51
CHEMBL26474 IC50 = 34.0 nM 7.47
CHEMBL312854 IC50 = 44.0 nM 7.36
CHEMBL315638 IC50 = 89.0 nM 7.05
CHEMBL315175 IC50 = 131.0 nM 6.88
CHEMBL315788 IC50 = 178.0 nM 6.75
CHEMBL88019 IC50 = 440.0 nM 6.36
CHEMBL315805 IC50 = 810.0 nM 6.09
CHEMBL86965 IC50 = 825.0 nM 6.08
CHEMBL86821 IC50 = 953.0 nM 6.02
CHEMBL315087 IC50 = 2045.0 nM 5.69