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Assay Detail

CHEMBL673746

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Functional
In vitro inhibitory potency for preventing sarafotoxin S6c induced constriction of rat tracheal rings (ETB receptor)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Trachea
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Bis-sulfonamides as endothelin receptor antagonists.
Boss C, Bolli MH, Weller T, Fischli W, Clozel M.
Bioorg Med Chem Lett (2003) 13 : 951 -954
PubMed 12617928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 16 7.02 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367444 1 8.04
CHEMBL172297 1 7.95
CHEMBL176997 1 7.48
CHEMBL173201 1 7.46
CHEMBL277275 1 7.41
CHEMBL367443 1 7.31
CHEMBL367274 1 7.30
CHEMBL177538 1 7.16
CHEMBL172030 1 7.15
CHEMBL368107 1 6.97
CHEMBL369676 1 6.62
CHEMBL172071 1 6.57
CHEMBL177802 1 6.57
CHEMBL171950 1 6.44
CHEMBL367958 1 6.36
CHEMBL368738 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367444 Kd = 9.12 nM 8.04
CHEMBL172297 Kd = 11.22 nM 7.95
CHEMBL176997 Kd = 33.11 nM 7.48
CHEMBL173201 Kd = 34.67 nM 7.46
CHEMBL277275 Kd = 38.9 nM 7.41
CHEMBL367443 Kd = 48.98 nM 7.31
CHEMBL367274 Kd = 50.12 nM 7.30
CHEMBL177538 Kd = 69.18 nM 7.16
CHEMBL172030 Kd = 70.79 nM 7.15
CHEMBL368107 Kd = 107.15 nM 6.97
CHEMBL369676 Kd = 239.88 nM 6.62
CHEMBL172071 Kd = 269.15 nM 6.57
CHEMBL177802 Kd = 269.15 nM 6.57
CHEMBL171950 Kd = 363.08 nM 6.44
CHEMBL367958 Kd = 436.52 nM 6.36
CHEMBL368738 Kd = 2630.27 nM 5.58