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Assay Detail

CHEMBL672490

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

Binding
Binding affinity towards Dopamine receptor D2 from mammalian clones expressed in CHO cell membranes using 2 (86.1 Ci/mmol,1.7nanoM)as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Ennis MD, Baze ME, Smith MW, Lawson CF, McCall RB, Lahti RA, Piercey MF.
J Med Chem (1992) 35 : 3058 -3066
PubMed 1323682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.99 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101535 1 8.82
CHEMBL320880 1 8.74
CHEMBL323088 1 8.70
CHEMBL102175 1 8.24
CHEMBL318166 1 8.24
CHEMBL418802 1 8.17
CHEMBL318374 1 7.80
CHEMBL103983 1 7.39
CHEMBL106283 1 7.24
CHEMBL319023 1 6.59
CHEMBL101483 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101535 Ki = 1.5 nM 8.82
CHEMBL320880 Ki = 1.8 nM 8.74
CHEMBL323088 Ki = 2.0 nM 8.70
CHEMBL102175 Ki = 5.7 nM 8.24
CHEMBL318166 Ki = 5.8 nM 8.24
CHEMBL418802 Ki = 6.7 nM 8.17
CHEMBL318374 Ki = 15.9 nM 7.80
CHEMBL103983 Ki = 41.0 nM 7.39
CHEMBL106283 Ki = 58.0 nM 7.24
CHEMBL319023 Ki = 255.0 nM 6.59
CHEMBL101483 Ki > 388.0 nM -