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Assay Detail

CHEMBL677401

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Binding
Effective concentration against Endothelin B receptor from rat cerebellum
30
Total Activities
29
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

Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
Doherty AM, Cody WL, DePue PL, He JX, Waite LA, Leonard DM, Leitz NL, Dudley DT, Rapundalo ST, Hingorani GP.
J Med Chem (1993) 36 : 2585 -2594
PubMed 8410970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.13 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313984 2 7.70
CHEMBL327350 1 7.44
CHEMBL1788127 1 7.16
CHEMBL313760 1 7.16
CHEMBL89736 1 6.82
CHEMBL85341 1 6.60
CHEMBL406279 1 6.54
CHEMBL313382 1 6.35
CHEMBL87243 1 6.35
CHEMBL313056 1 6.08
CHEMBL315047 1 5.72
CHEMBL86814 1 5.70
CHEMBL2370070 1 5.61
CHEMBL87252 1 5.58
CHEMBL315328 1 5.58
CHEMBL316092 1 5.34
CHEMBL289687 1 5.04
CHEMBL315658 1 5.03
CHEMBL315780 1 5.01
CHEMBL273391 1 4.73
CHEMBL315384 1 -
CHEMBL431218 1 -
CHEMBL431874 1 -
CHEMBL87724 1 -
CHEMBL86737 1 -
CHEMBL312916 1 -
CHEMBL314239 1 -
CHEMBL330489 1 -
CHEMBL89416 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313984 IC50 = 20.0 nM 7.70
CHEMBL327350 IC50 = 36.0 nM 7.44
CHEMBL313984 IC50 = 60.0 nM 7.22
CHEMBL1788127 IC50 = 70.0 nM 7.16
CHEMBL313760 IC50 = 70.0 nM 7.16
CHEMBL89736 IC50 = 150.0 nM 6.82
CHEMBL85341 IC50 = 250.0 nM 6.60
CHEMBL406279 IC50 = 290.0 nM 6.54
CHEMBL87243 IC50 = 450.0 nM 6.35
CHEMBL313382 IC50 = 450.0 nM 6.35
CHEMBL313056 IC50 = 840.0 nM 6.08
CHEMBL315047 IC50 = 1900.0 nM 5.72
CHEMBL86814 IC50 = 2000.0 nM 5.70
CHEMBL2370070 IC50 = 2450.0 nM 5.61
CHEMBL87252 IC50 = 2600.0 nM 5.58
CHEMBL315328 IC50 = 2600.0 nM 5.58
CHEMBL316092 IC50 = 4600.0 nM 5.34
CHEMBL289687 IC50 = 9100.0 nM 5.04
CHEMBL315658 IC50 = 9300.0 nM 5.03
CHEMBL315780 IC50 = 9800.0 nM 5.01
CHEMBL273391 IC50 = 18500.0 nM 4.73
CHEMBL312916 IC50 > 10000.0 nM -
CHEMBL86737 IC50 > 10000.0 nM -
CHEMBL431874 IC50 > 10000.0 nM -
CHEMBL431218 IC50 > 10000.0 nM -
CHEMBL315384 IC50 > 10000.0 nM -
CHEMBL87724 IC50 > 10000.0 nM -
CHEMBL314239 IC50 > 10000.0 nM -
CHEMBL330489 IC50 > 10000.0 nM -
CHEMBL89416 IC50 > 10000.0 nM -