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Assay Detail

CHEMBL971387

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

Binding
Displacement of [3H]spiperone from rat dopamine D3 receptor expressed in HEK293 cells
21
Total Activities
15
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(3) dopamine receptor (CHEMBL3138)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Bioisosteric heterocyclic versions of 7-{[2-(4-phenyl-piperazin-1-yl)ethyl]propylamino}-5,6,7,8-tetrahydronaphthalen-2-ol: identification of highly potent and selective agonists for dopamine D3 receptor with potent in vivo activity.
Biswas S, Hazeldine S, Ghosh B, Parrington I, Kuzhikandathil E, Reith ME, Dutta AK.
J Med Chem (2008) 51 : 3005 -3019
PubMed 18410082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.83 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467540 1 9.04
CHEMBL156639 1 8.81
CHEMBL468017 3 8.74
CHEMBL285755 1 8.63
CHEMBL468015 3 8.38
CHEMBL468016 3 8.29
CHEMBL468833 1 8.15
CHEMBL468022 1 7.91
CHEMBL513352 1 7.46
CHEMBL467767 1 7.39
CHEMBL468834 1 7.33
CHEMBL469181 1 6.81
CHEMBL466561 1 6.80
CHEMBL467768 1 6.73
CHEMBL469182 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467540 Ki = 0.92 nM 9.04
CHEMBL156639 Ki = 1.56 nM 8.81
CHEMBL468017 Ki = 1.8 nM 8.74
CHEMBL468017 Ki = 1.82 nM 8.74
CHEMBL285755 Ki = 2.35 nM 8.63
CHEMBL468015 Ki = 4.15 nM 8.38
CHEMBL468016 Ki = 5.09 nM 8.29
CHEMBL468015 Ki = 5.96 nM 8.22
CHEMBL468016 Ki = 7.01 nM 8.15
CHEMBL468833 Ki = 7.1 nM 8.15
CHEMBL468017 Ki = 12.0 nM 7.92
CHEMBL468022 Ki = 12.4 nM 7.91
CHEMBL513352 Ki = 34.8 nM 7.46
CHEMBL467767 Ki = 40.7 nM 7.39
CHEMBL468015 Ki = 44.0 nM 7.36
CHEMBL468834 Ki = 46.7 nM 7.33
CHEMBL468016 Ki = 101.0 nM 7.00
CHEMBL469181 Ki = 155.0 nM 6.81
CHEMBL466561 Ki = 160.0 nM 6.80
CHEMBL467768 Ki = 188.0 nM 6.73
CHEMBL469182 Ki = 254.0 nM 6.59