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Assay Detail

CHEMBL774074

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

Functional
Ability to stimulate peripheral prejunctional dopaminergic receptors by 50% inhibition of vasoconstrictor response to field stimulation in isolated perfused rabbit ear artery
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Syntheses and in vitro evaluation of 4-(2-aminoethyl)-2(3H)-indolones and related compounds as peripheral prejunctional dopamine receptor agonists.
DeMarinis RM, Gallagher G, Hall RF, Franz RG, Webster C, Huffman WF, Schwartz MS, Kaiser C, Ross ST, Wilson JW.
J Med Chem (1986) 29 : 939 -947
PubMed 3712384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.99 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL587 SKF-89124A 1 8.70
CHEMBL174011 1 7.75
CHEMBL172846 1 7.55
CHEMBL366579 1 7.28
CHEMBL59 DOPAMINE 4.0 1 7.14
CHEMBL176858 1 7.10
CHEMBL589 ROPINIROLE 4.0 1 7.00
CHEMBL278188 1 6.94
CHEMBL367076 1 6.66
CHEMBL39845 1 6.16
CHEMBL173227 1 6.12
CHEMBL368590 1 5.52
CHEMBL353386 1 -
CHEMBL173979 1 -
CHEMBL170703 1 -
CHEMBL173855 1 -
CHEMBL172980 1 -
CHEMBL369274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL587 SKF-89124A EC50 = 2.0 nM 8.70
CHEMBL174011 EC50 = 18.0 nM 7.75
CHEMBL172846 EC50 = 28.0 nM 7.55
CHEMBL366579 EC50 = 53.0 nM 7.28
CHEMBL59 DOPAMINE EC50 = 73.0 nM 7.14
CHEMBL176858 EC50 = 80.0 nM 7.10
CHEMBL589 ROPINIROLE EC50 = 100.0 nM 7.00
CHEMBL278188 EC50 = 116.0 nM 6.94
CHEMBL367076 EC50 = 218.0 nM 6.66
CHEMBL39845 EC50 = 700.0 nM 6.16
CHEMBL173227 EC50 = 750.0 nM 6.12
CHEMBL368590 EC50 = 3000.0 nM 5.52
CHEMBL353386 EC50 > 3000.0 nM -
CHEMBL173979 EC50 > 3000.0 nM -
CHEMBL170703 EC50 > 3000.0 nM -
CHEMBL173855 EC50 > 3000.0 nM -
CHEMBL172980 EC50 > 3000.0 nM -
CHEMBL369274 EC50 > 10000.0 nM -