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Assay Detail

CHEMBL671959

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

Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
11
Total Activities
11
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

Evaluation of cis- and trans-9- and 11-hydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridines as structurally rigid, selective D1 dopamine receptor ligands.
Brewster WK, Nichols DE, Watts VJ, Riggs RM, Mottola D, Mailman RB.
J Med Chem (1995) 38 : 318 -327
PubMed 7830274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.76 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62 SCH-23390 1 9.24
CHEMBL71 CHLORPROMAZINE 4.0 1 8.67
CHEMBL25856 DIHYDREXIDINE 2.0 1 8.15
CHEMBL113477 1 6.99
CHEMBL111348 1 6.94
CHEMBL68680 1 6.49
CHEMBL321040 1 6.28
CHEMBL418791 1 6.02
CHEMBL320481 1 5.54
CHEMBL113053 1 5.26
CHEMBL326781 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62 SCH-23390 IC50 = 0.57 nM 9.24
CHEMBL71 CHLORPROMAZINE IC50 = 2.15 nM 8.67
CHEMBL25856 DIHYDREXIDINE IC50 = 7.15 nM 8.15
CHEMBL113477 IC50 = 102.0 nM 6.99
CHEMBL111348 IC50 = 115.0 nM 6.94
CHEMBL68680 IC50 = 322.0 nM 6.49
CHEMBL321040 IC50 = 529.0 nM 6.28
CHEMBL418791 IC50 = 955.0 nM 6.02
CHEMBL320481 IC50 = 2900.0 nM 5.54
CHEMBL113053 IC50 = 5550.0 nM 5.26
CHEMBL326781 IC50 = 16700.0 nM 4.78