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Assay Detail

CHEMBL675667

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

Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D3 expressed on CHO K-1 cells.
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.
van Vliet LA, Tepper PG, Dijkstra D, Damsma G, Wikström H, Pugsley TA, Akunne HC, Heffner TG, Glase SA, Wise LD.
J Med Chem (1996) 39 : 4233 -4237
PubMed 8863800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.47 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269004 1 9.27
CHEMBL301559 1 9.24
CHEMBL336652 1 9.18
CHEMBL134571 1 9.15
CHEMBL335392 1 9.13
CHEMBL135954 1 9.12
CHEMBL334472 1 9.12
CHEMBL94015 1 8.96
CHEMBL135932 1 8.85
CHEMBL7806 1 8.74
CHEMBL134747 1 8.70
CHEMBL109684 1 8.47
CHEMBL1303 ROTIGOTINE 4.0 1 8.40
CHEMBL133830 1 8.29
CHEMBL305706 1 7.24
CHEMBL15146 1 7.12
CHEMBL336295 1 6.95
CHEMBL135152 1 6.87
CHEMBL133938 1 6.81
CHEMBL132261 1 6.68
CHEMBL135944 1 6.58
CHEMBL441092 1 6.46
CHEMBL134866 1 6.44
CHEMBL135048 1 6.39
CHEMBL134759 1 6.30
CHEMBL11615 1 6.28
CHEMBL131851 1 6.22
CHEMBL134326 1 6.19
CHEMBL30560 1 6.17
CHEMBL134701 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269004 Ki = 0.54 nM 9.27
CHEMBL301559 Ki = 0.57 nM 9.24
CHEMBL336652 Ki = 0.66 nM 9.18
CHEMBL134571 Ki = 0.71 nM 9.15
CHEMBL335392 Ki = 0.74 nM 9.13
CHEMBL135954 Ki = 0.75 nM 9.12
CHEMBL334472 Ki = 0.75 nM 9.12
CHEMBL94015 Ki = 1.1 nM 8.96
CHEMBL135932 Ki = 1.41 nM 8.85
CHEMBL7806 Ki = 1.82 nM 8.74
CHEMBL134747 Ki = 1.98 nM 8.70
CHEMBL109684 Ki = 3.37 nM 8.47
CHEMBL1303 ROTIGOTINE Ki = 3.99 nM 8.40
CHEMBL133830 Ki = 5.12 nM 8.29
CHEMBL305706 Ki = 58.0 nM 7.24
CHEMBL15146 Ki = 76.0 nM 7.12
CHEMBL336295 Ki = 113.0 nM 6.95
CHEMBL135152 Ki = 136.0 nM 6.87
CHEMBL133938 Ki = 154.0 nM 6.81
CHEMBL132261 Ki = 211.0 nM 6.68
CHEMBL135944 Ki = 266.0 nM 6.58
CHEMBL441092 Ki = 343.0 nM 6.46
CHEMBL134866 Ki = 361.0 nM 6.44
CHEMBL135048 Ki = 409.0 nM 6.39
CHEMBL134759 Ki = 501.0 nM 6.30
CHEMBL11615 Ki = 529.0 nM 6.28
CHEMBL131851 Ki = 603.0 nM 6.22
CHEMBL134326 Ki = 648.0 nM 6.19
CHEMBL30560 Ki = 683.0 nM 6.17
CHEMBL134701 Ki = 857.0 nM 6.07
CHEMBL335971 Ki = 1372.0 nM 5.86
CHEMBL422274 Ki = 2220.0 nM 5.65
CHEMBL336962 Ki = 3055.0 nM 5.51