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Assay Detail

CHEMBL770659

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Ability to relax the electrically stimulated rabbit ear artery was determined
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Synthesis and evaluation of non-catechol D-1 and D-2 dopamine receptor agonists: benzimidazol-2-one, benzoxazol-2-one, and the highly potent benzothiazol-2-one 7-ethylamines.
Weinstock J, Gaitanopoulos DE, Stringer OD, Franz RG, Hieble JP, Kinter LB, Mann WA, Flaim KE, Gessner G.
J Med Chem (1987) 30 : 1166 -1176
PubMed 2955118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.62 10.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17231 1 10.55
CHEMBL587 SKF-89124A 1 8.74
CHEMBL17550 1 8.22
CHEMBL279106 1 8.15
CHEMBL275155 1 8.10
CHEMBL275600 1 8.05
CHEMBL418548 1 7.55
CHEMBL17357 1 7.52
CHEMBL17872 1 7.30
CHEMBL59 DOPAMINE 4.0 1 7.12
CHEMBL15564 1 7.10
CHEMBL589 ROPINIROLE 4.0 1 7.00
CHEMBL278188 1 6.94
CHEMBL441220 1 6.00
CHEMBL588 FENOLDOPAM 4.0 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17231 EC50 = 0.028 nM 10.55
CHEMBL587 SKF-89124A EC50 = 1.8 nM 8.74
CHEMBL17550 EC50 = 6.0 nM 8.22
CHEMBL279106 EC50 = 7.0 nM 8.15
CHEMBL275155 EC50 = 8.0 nM 8.10
CHEMBL275600 EC50 = 9.0 nM 8.05
CHEMBL418548 EC50 = 28.0 nM 7.55
CHEMBL17357 EC50 = 30.0 nM 7.52
CHEMBL17872 EC50 = 50.0 nM 7.30
CHEMBL59 DOPAMINE EC50 = 76.0 nM 7.12
CHEMBL15564 EC50 = 80.0 nM 7.10
CHEMBL589 ROPINIROLE EC50 = 100.0 nM 7.00
CHEMBL278188 EC50 = 116.0 nM 6.94
CHEMBL441220 EC50 = 1000.0 nM 6.00
CHEMBL588 FENOLDOPAM EC50 = 1200.0 nM 5.92