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Assay Detail

CHEMBL670883

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

Binding
In vitro binding affinity towards cloned human Dopamine receptor D2A using [3H]- Raclopride as radioligand.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.
Linnanen T, Brisander M, Mohell N, Johansson AM.
Bioorg Med Chem Lett (2001) 11 : 367 -370
PubMed 11212112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.52 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 7.38
CHEMBL253319 1 7.26
CHEMBL284586 1 7.08
CHEMBL124419 1 6.58
CHEMBL122453 1 6.49
CHEMBL122485 1 6.27
CHEMBL120927 1 5.88
CHEMBL253318 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE Ki = 41.6 nM 7.38
CHEMBL253319 Ki = 54.6 nM 7.26
CHEMBL284586 Ki = 83.2 nM 7.08
CHEMBL124419 Ki = 265.0 nM 6.58
CHEMBL122453 Ki = 327.0 nM 6.49
CHEMBL122485 Ki = 541.0 nM 6.27
CHEMBL120927 Ki = 1330.0 nM 5.88
CHEMBL253318 Ki = 6110.0 nM 5.21