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Assay Detail

CHEMBL672685

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

Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analogue.
Neumeyer JL, Kula NS, Baldessarini RJ, Baindur N.
J Med Chem (1992) 35 : 1466 -1471
PubMed 1533424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.07 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34095 1 8.37
CHEMBL35354 1 8.29
CHEMBL284473 1 8.09
CHEMBL32145 1 8.00
CHEMBL288090 1 7.71
CHEMBL24077 (R)-SKF-38393 1 7.30
CHEMBL286080 SKF-38393 1 6.72
CHEMBL286424 1 5.73
CHEMBL286120 1 5.55
CHEMBL284746 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34095 IC50 = 4.3 nM 8.37
CHEMBL35354 IC50 = 5.1 nM 8.29
CHEMBL284473 IC50 = 8.1 nM 8.09
CHEMBL32145 IC50 = 10.1 nM 8.00
CHEMBL288090 IC50 = 19.7 nM 7.71
CHEMBL24077 (R)-SKF-38393 IC50 = 50.0 nM 7.30
CHEMBL286080 SKF-38393 IC50 = 190.0 nM 6.72
CHEMBL286424 IC50 = 1880.0 nM 5.73
CHEMBL286120 IC50 = 2800.0 nM 5.55
CHEMBL284746 IC50 = 10700.0 nM 4.97