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Assay Detail

CHEMBL670880

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

Binding
Displacement of [3H]raclopride from human Dopamine receptor D2A
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.
Hedberg MH, Linnanen T, Jansen JM, Nordvall G, Hjorth S, Unelius L, Johansson AM.
J Med Chem (1996) 39 : 3503 -3513
PubMed 8784448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.81 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27559 1 7.90
CHEMBL53 APOMORPHINE 4.0 1 7.38
CHEMBL119455 1 7.23
CHEMBL118254 1 7.10
CHEMBL119656 1 6.75
CHEMBL115969 1 6.74
CHEMBL333836 1 6.71
CHEMBL27940 1 6.70
CHEMBL25924 1 6.63
CHEMBL281357 1 6.28
CHEMBL117841 1 6.26
CHEMBL115402 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27559 Ki = 12.7 nM 7.90
CHEMBL53 APOMORPHINE Ki = 41.9 nM 7.38
CHEMBL119455 Ki = 58.5 nM 7.23
CHEMBL118254 Ki = 79.2 nM 7.10
CHEMBL119656 Ki = 177.0 nM 6.75
CHEMBL115969 Ki = 183.0 nM 6.74
CHEMBL333836 Ki = 195.0 nM 6.71
CHEMBL27940 Ki = 201.0 nM 6.70
CHEMBL25924 Ki = 233.0 nM 6.63
CHEMBL281357 Ki = 527.0 nM 6.28
CHEMBL117841 Ki = 551.0 nM 6.26
CHEMBL115402 Ki = 1000.0 nM 6.00