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Assay Detail

CHEMBL894060

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

Binding
Displacement of [3H]spiroperidol from human recombinant Dopamine D2 long receptor
26
Total Activities
26
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

Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2.
Leopoldo M, Lacivita E, Contino M, Colabufo NA, Berardi F, Perrone R.
J Med Chem (2007) 50 : 4214 -4221
PubMed 17649988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.05 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.70
CHEMBL225284 1 8.14
CHEMBL243744 1 7.82
CHEMBL224820 1 7.58
CHEMBL243955 1 7.50
CHEMBL222477 1 7.29
CHEMBL243743 1 7.22
CHEMBL389718 1 7.17
CHEMBL244161 1 6.97
CHEMBL243742 1 6.91
CHEMBL222755 1 6.84
CHEMBL243523 1 6.76
CHEMBL243954 1 6.65
CHEMBL221513 1 6.58
CHEMBL244577 1 6.54
CHEMBL225571 1 6.17
CHEMBL225512 1 6.01
CHEMBL222188 1 6.00
CHEMBL222489 1 -
CHEMBL387738 1 -
CHEMBL243953 1 -
CHEMBL244162 1 -
CHEMBL389110 1 -
CHEMBL390015 1 -
CHEMBL390213 1 -
CHEMBL244792 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.0 nM 8.70
CHEMBL225284 Ki = 7.3 nM 8.14
CHEMBL243744 Ki = 15.0 nM 7.82
CHEMBL224820 Ki = 26.4 nM 7.58
CHEMBL243955 Ki = 32.0 nM 7.50
CHEMBL222477 Ki = 51.0 nM 7.29
CHEMBL243743 Ki = 60.0 nM 7.22
CHEMBL389718 Ki = 68.0 nM 7.17
CHEMBL244161 Ki = 107.0 nM 6.97
CHEMBL243742 Ki = 123.0 nM 6.91
CHEMBL222755 Ki = 143.0 nM 6.84
CHEMBL243523 Ki = 173.0 nM 6.76
CHEMBL243954 Ki = 224.0 nM 6.65
CHEMBL221513 Ki = 265.0 nM 6.58
CHEMBL244577 Ki = 292.0 nM 6.54
CHEMBL225571 Ki = 681.0 nM 6.17
CHEMBL225512 Ki = 987.0 nM 6.01
CHEMBL222188 Ki = 1000.0 nM 6.00
CHEMBL222489 Ki > 1000.0 nM -
CHEMBL387738 Ki > 1000.0 nM -
CHEMBL243953 Ki > 1000.0 nM -
CHEMBL244162 Ki - -
CHEMBL389110 Ki > 1000.0 nM -
CHEMBL390015 Ki > 1000.0 nM -
CHEMBL390213 Ki > 1000.0 nM -
CHEMBL244792 Ki - -