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Assay Detail

CHEMBL664743

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

Binding
Binding affinity was measured on cloned Human D2A Receptor which is labeled by [3H]raclopride
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

Derivatives of (R)-1,11-methyleneaporphine: synthesis, structure, and interactions with G-protein coupled receptors.
Linnanen T, Brisander M, Unelius L, Sundholm G, Hacksell U, Johansson AM.
J Med Chem (2000) 43 : 1339 -1349
PubMed 10753471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.76 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282863 1 7.71
CHEMBL27132 1 7.41
CHEMBL53 APOMORPHINE 4.0 1 7.38
CHEMBL284586 1 7.08
CHEMBL27940 1 6.70
CHEMBL281357 1 6.28
CHEMBL26998 1 6.09
CHEMBL22778 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282863 Ki = 19.4 nM 7.71
CHEMBL27132 Ki = 39.2 nM 7.41
CHEMBL53 APOMORPHINE Ki = 41.6 nM 7.38
CHEMBL284586 Ki = 83.2 nM 7.08
CHEMBL27940 Ki = 201.0 nM 6.70
CHEMBL281357 Ki = 527.0 nM 6.28
CHEMBL26998 Ki = 819.0 nM 6.09
CHEMBL22778 Ki = 3760.0 nM 5.42