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Assay Detail

CHEMBL675445

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Binding
Binding affinity against Endothelin receptor from rat heart ventricle
31
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Endothelin receptor (CHEMBL2111453)
Type PROTEIN FAMILY
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 31 5.66 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313760 1 7.60
CHEMBL1788127 1 7.40
CHEMBL313382 1 6.89
CHEMBL313984 1 6.48
CHEMBL327350 1 6.42
CHEMBL85341 1 6.40
CHEMBL406279 1 6.38
CHEMBL2370070 1 6.17
CHEMBL86814 1 6.13
CHEMBL313056 1 6.13
CHEMBL315047 1 6.00
CHEMBL87243 1 5.79
CHEMBL315658 1 5.67
CHEMBL315780 1 5.42
CHEMBL289687 2 5.39
CHEMBL438194 1 5.36
CHEMBL262166 1 5.28
CHEMBL86737 1 5.17
CHEMBL431874 1 5.05
CHEMBL431218 1 4.92
CHEMBL315328 1 4.91
CHEMBL2370061 1 4.77
CHEMBL87724 1 4.61
CHEMBL2370073 1 4.43
CHEMBL2114215 1 4.41
CHEMBL432091 1 4.24
CHEMBL3350293 1 -
CHEMBL2369145 1 -
CHEMBL313122 1 -
CHEMBL314239 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313760 IC50 = 25.0 nM 7.60
CHEMBL1788127 IC50 = 40.0 nM 7.40
CHEMBL313382 IC50 = 130.0 nM 6.89
CHEMBL313984 IC50 = 330.0 nM 6.48
CHEMBL327350 IC50 = 380.0 nM 6.42
CHEMBL85341 IC50 = 400.0 nM 6.40
CHEMBL406279 IC50 = 420.0 nM 6.38
CHEMBL2370070 IC50 = 680.0 nM 6.17
CHEMBL86814 IC50 = 740.0 nM 6.13
CHEMBL313056 IC50 = 740.0 nM 6.13
CHEMBL315047 IC50 = 1000.0 nM 6.00
CHEMBL87243 IC50 = 1610.0 nM 5.79
CHEMBL315658 IC50 = 2150.0 nM 5.67
CHEMBL315780 IC50 = 3800.0 nM 5.42
CHEMBL289687 IC50 = 4100.0 nM 5.39
CHEMBL438194 IC50 = 4400.0 nM 5.36
CHEMBL289687 IC50 = 4500.0 nM 5.35
CHEMBL262166 IC50 = 5200.0 nM 5.28
CHEMBL86737 IC50 = 6830.0 nM 5.17
CHEMBL431874 IC50 = 9000.0 nM 5.05
CHEMBL431218 IC50 = 12000.0 nM 4.92
CHEMBL315328 IC50 = 12400.0 nM 4.91
CHEMBL2370061 IC50 = 16900.0 nM 4.77
CHEMBL87724 IC50 = 24500.0 nM 4.61
CHEMBL2370073 IC50 = 37000.0 nM 4.43
CHEMBL2114215 IC50 = 39000.0 nM 4.41
CHEMBL432091 IC50 = 58000.0 nM 4.24
CHEMBL3350293 IC50 = 169000.0 nM -
CHEMBL2369145 IC50 > 50000.0 nM -
CHEMBL313122 IC50 > 50000.0 nM -
CHEMBL314239 IC50 > 50000.0 nM -