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Assay Detail

CHEMBL2213380

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

Binding
Displacement of [3H]spiperone from rat cloned dopamine D2L receptor expressed in HEK-293 cells by competition binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.
Gogoi S, Biswas S, Modi G, Antonio T, Reith ME, Dutta AK.
ACS Med Chem Lett (2012) 3 : 991 -996
PubMed 23275802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206265 1 8.70
CHEMBL2206264 1 8.60
CHEMBL2206273 1 8.41
CHEMBL2206272 1 8.23
CHEMBL2206266 1 7.96
CHEMBL2206269 1 7.80
CHEMBL2206267 1 7.26
CHEMBL269004 1 7.23
CHEMBL2203317 1 7.16
CHEMBL2206270 1 7.16
CHEMBL2206271 1 7.12
CHEMBL2206268 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206265 Ki = 2.0 nM 8.70
CHEMBL2206264 Ki = 2.5 nM 8.60
CHEMBL2206273 Ki = 3.9 nM 8.41
CHEMBL2206272 Ki = 5.9 nM 8.23
CHEMBL2206266 Ki = 11.0 nM 7.96
CHEMBL2206269 Ki = 16.0 nM 7.80
CHEMBL2206267 Ki = 55.0 nM 7.26
CHEMBL269004 Ki = 59.0 nM 7.23
CHEMBL2203317 Ki = 69.0 nM 7.16
CHEMBL2206270 Ki = 70.0 nM 7.16
CHEMBL2206271 Ki = 75.0 nM 7.12
CHEMBL2206268 Ki = 140.0 nM 6.85