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Assay Detail

CHEMBL672344

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Binding
Binding affinity towards dopamine receptor D2 in rat striatal membranes
30
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

trans-4-[4-(Methoxyphenyl)cyclohexyl]-1-arylpiperazines: a new class of potent and selective 5-HT(1A) receptor ligands as conformationally constrained analogues of 4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]-1-arylpiperazines.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Lacivita E, Tortorella V, Leonardi A, Poggesi E, Testa R.
J Med Chem (2001) 44 : 4431 -4442
PubMed 11728188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 6.27 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 9.10
CHEMBL2112776 2 7.16
CHEMBL444590 1 6.93
CHEMBL140406 1 6.90
CHEMBL2112773 2 6.61
CHEMBL138289 1 6.49
CHEMBL138109 1 6.42
CHEMBL139505 1 6.35
CHEMBL2112774 2 6.23
CHEMBL2112779 2 6.17
CHEMBL344146 1 6.12
CHEMBL2112771 2 6.10
CHEMBL2112780 2 6.04
CHEMBL140287 1 5.91
CHEMBL423181 1 5.76
CHEMBL2112778 2 5.66
CHEMBL139848 1 5.66
CHEMBL138892 1 5.53
CHEMBL139146 1 -
CHEMBL344432 1 -
CHEMBL136563 1 -
CHEMBL138899 1 -
CHEMBL138900 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 0.8 nM 9.10
CHEMBL2112776 Ki = 70.0 nM 7.16
CHEMBL444590 Ki = 117.0 nM 6.93
CHEMBL140406 Ki = 125.0 nM 6.90
CHEMBL2112773 Ki = 243.0 nM 6.61
CHEMBL138289 Ki = 327.0 nM 6.49
CHEMBL138109 Ki = 378.0 nM 6.42
CHEMBL139505 Ki = 450.0 nM 6.35
CHEMBL2112774 Ki = 586.0 nM 6.23
CHEMBL2112779 Ki = 668.0 nM 6.17
CHEMBL344146 Ki = 750.0 nM 6.12
CHEMBL2112774 Ki = 783.0 nM 6.11
CHEMBL2112771 Ki = 787.0 nM 6.10
CHEMBL2112771 Ki = 792.0 nM 6.10
CHEMBL2112780 Ki = 910.0 nM 6.04
CHEMBL2112779 Ki = 910.0 nM 6.04
CHEMBL140287 Ki = 1220.0 nM 5.91
CHEMBL2112776 Ki = 1310.0 nM 5.88
CHEMBL423181 Ki = 1730.0 nM 5.76
CHEMBL2112773 Ki = 2120.0 nM 5.67
CHEMBL139848 Ki = 2190.0 nM 5.66
CHEMBL2112778 Ki = 2190.0 nM 5.66
CHEMBL2112780 Ki = 2380.0 nM 5.62
CHEMBL138892 Ki = 2930.0 nM 5.53
CHEMBL344432 Ki > 850.0 nM -
CHEMBL138899 Ki > 850.0 nM -
CHEMBL2112778 Ki > 850.0 nM -
CHEMBL136563 Ki > 850.0 nM -
CHEMBL138900 Ki > 850.0 nM -
CHEMBL139146 Ki > 850.0 nM -