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Assay Detail

CHEMBL676488

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Functional
In vitro inhibitory potency for preventing ET-1 induced constriction of rat aortic rings (ETA receptor)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL4566)
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 15 6.38 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367958 1 7.02
CHEMBL177802 1 6.98
CHEMBL367444 1 6.92
CHEMBL177538 1 6.61
CHEMBL368738 1 6.61
CHEMBL171950 1 6.54
CHEMBL368617 1 6.52
CHEMBL367443 1 6.51
CHEMBL172071 1 6.46
CHEMBL172297 1 6.16
CHEMBL369676 1 6.08
CHEMBL172030 1 6.08
CHEMBL176997 1 5.50
CHEMBL368107 1 5.32
CHEMBL173201 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367958 Kd = 95.5 nM 7.02
CHEMBL177802 Kd = 104.71 nM 6.98
CHEMBL367444 Kd = 120.23 nM 6.92
CHEMBL177538 Kd = 245.47 nM 6.61
CHEMBL368738 Kd = 245.47 nM 6.61
CHEMBL171950 Kd = 288.4 nM 6.54
CHEMBL368617 Kd = 302.0 nM 6.52
CHEMBL367443 Kd = 309.03 nM 6.51
CHEMBL172071 Kd = 346.74 nM 6.46
CHEMBL172297 Kd = 691.83 nM 6.16
CHEMBL369676 Kd = 831.76 nM 6.08
CHEMBL172030 Kd = 831.76 nM 6.08
CHEMBL176997 Kd = 3162.28 nM 5.50
CHEMBL368107 Kd = 4786.3 nM 5.32
CHEMBL173201 Kd > 10000.0 nM -