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Assay Detail

CHEMBL671553

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Binding
Binding affinity against endothelin B receptor rat cerebellar membranes.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.
Cody WL, He JX, DePue PL, Waite LA, Leonard DM, Sefler AM, Kaltenbronn JS, Haleen SJ, Walker DM, Flynn MA.
J Med Chem (1995) 38 : 2809 -2819
PubMed 7636842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.43 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405599 — — 1 8.00
CHEMBL385492 — — 1 7.92
CHEMBL262993 — — 1 7.82
CHEMBL319719 — — 1 7.80
CHEMBL317099 — — 1 7.70
CHEMBL384052 — — 1 7.52
CHEMBL216082 — — 1 7.48
CHEMBL2370255 — — 1 7.48
CHEMBL319660 — — 1 7.29
CHEMBL97470 — — 1 7.28
CHEMBL265116 — — 1 7.25
CHEMBL433349 — — 1 7.22
CHEMBL384728 — — 1 7.10
CHEMBL433406 — — 1 6.85
CHEMBL94983 — — 1 6.82
CHEMBL265734 — — 1 6.72
CHEMBL263295 — — 1 6.68
CHEMBL96822 — — 1 6.58
CHEMBL323331 — — 1 6.58
CHEMBL94907 — — 1 6.48
CHEMBL414082 — — 1 6.46
CHEMBL264579 — — 1 6.41
CHEMBL262229 — — 1 6.40
CHEMBL386181 — — 1 6.22
CHEMBL413179 — — 1 6.20
CHEMBL330144 — — 1 6.14
CHEMBL97431 — — 1 6.14
CHEMBL411797 — — 1 6.13
CHEMBL407933 — — 1 5.89
CHEMBL415238 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405599 — IC50 = 10.0 nM 8.00
CHEMBL385492 — IC50 = 12.0 nM 7.92
CHEMBL262993 — IC50 = 15.0 nM 7.82
CHEMBL319719 — IC50 = 16.0 nM 7.80
CHEMBL317099 — IC50 = 20.0 nM 7.70
CHEMBL384052 — IC50 = 30.0 nM 7.52
CHEMBL216082 — IC50 = 33.0 nM 7.48
CHEMBL2370255 — IC50 = 33.0 nM 7.48
CHEMBL319660 — IC50 = 51.0 nM 7.29
CHEMBL97470 — IC50 = 52.0 nM 7.28
CHEMBL265116 — IC50 = 56.0 nM 7.25
CHEMBL433349 — IC50 = 60.0 nM 7.22
CHEMBL384728 — IC50 = 80.0 nM 7.10
CHEMBL433406 — IC50 = 140.0 nM 6.85
CHEMBL94983 — IC50 = 150.0 nM 6.82
CHEMBL265734 — IC50 = 190.0 nM 6.72
CHEMBL263295 — IC50 = 210.0 nM 6.68
CHEMBL96822 — IC50 = 260.0 nM 6.58
CHEMBL323331 — IC50 = 260.0 nM 6.58
CHEMBL94907 — IC50 = 330.0 nM 6.48
CHEMBL414082 — IC50 = 350.0 nM 6.46
CHEMBL264579 — IC50 = 390.0 nM 6.41
CHEMBL262229 — IC50 = 400.0 nM 6.40
CHEMBL386181 — IC50 = 600.0 nM 6.22
CHEMBL413179 — IC50 = 630.0 nM 6.20
CHEMBL330144 — IC50 = 730.0 nM 6.14
CHEMBL97431 — IC50 = 730.0 nM 6.14
CHEMBL411797 — IC50 = 740.0 nM 6.13
CHEMBL407933 — IC50 = 1300.0 nM 5.89
CHEMBL415238 — IC50 = 1300.0 nM 5.89
CHEMBL2370247 — IC50 = 1600.0 nM 5.80
CHEMBL319537 — IC50 = 1900.0 nM 5.72
CHEMBL327523 — IC50 = 2000.0 nM 5.70
CHEMBL94689 — IC50 = 2400.0 nM 5.62
CHEMBL94525 — IC50 = 3700.0 nM 5.43
CHEMBL431433 — IC50 = 4700.0 nM 5.33
CHEMBL329609 — IC50 = 5000.0 nM 5.30
CHEMBL405178 — IC50 = 5900.0 nM 5.23
CHEMBL318020 — IC50 = 6000.0 nM 5.22
CHEMBL2370254 — IC50 = 6100.0 nM 5.21
CHEMBL2370253 — IC50 = 6800.0 nM 5.17
CHEMBL405709 — IC50 = 7500.0 nM 5.12
CHEMBL269428 — IC50 = 10000.0 nM 5.00
CHEMBL327590 — IC50 > 10000.0 nM -
CHEMBL2370246 — IC50 > 10000.0 nM -
CHEMBL94730 — IC50 > 10000.0 nM -
CHEMBL2370245 — IC50 > 1000.0 nM -
CHEMBL439435 — IC50 > 10000.0 nM -
CHEMBL329170 — IC50 > 10000.0 nM -
CHEMBL2370252 — IC50 > 10000.0 nM -