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Assay Detail

CHEMBL678341

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

Binding
Affinity against the dopamine receptor D2 using [3H]spiperinone.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-aryl-N'-benzylpiperazines as potential antipsychotic agents.
Reitz AB, Baxter EW, Bennett DJ, Codd EE, Jordan AD, Malloy EA, Maryanoff BE, McDonnell ME, Ortegon ME, Renzi MJ.
J Med Chem (1995) 38 : 4211 -4222
PubMed 7473548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.53 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428175 RWJ-25730 1 9.10
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL10085 MAZAPERTINE 2.0 1 8.66
CHEMBL135135 1 8.30
CHEMBL134304 1 7.80
CHEMBL1161079 1 7.77
CHEMBL423712 1 7.70
CHEMBL1161087 1 7.66
CHEMBL443546 1 7.64
CHEMBL275045 1 7.64
CHEMBL1161096 1 7.55
CHEMBL334767 1 7.51
CHEMBL1161088 1 7.51
CHEMBL3392290 1 7.50
CHEMBL10105 1 7.34
CHEMBL135676 1 7.29
CHEMBL1161120 1 7.28
CHEMBL341402 1 7.25
CHEMBL1161083 1 7.24
CHEMBL1161076 1 7.20
CHEMBL1161078 1 7.19
CHEMBL340268 1 7.06
CHEMBL135107 1 7.05
CHEMBL135938 1 7.05
CHEMBL416703 1 6.92
CHEMBL135129 1 6.70
CHEMBL439607 1 6.52
CHEMBL134951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428175 RWJ-25730 Ki = 0.8 nM 9.10
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL10085 MAZAPERTINE Ki = 2.2 nM 8.66
CHEMBL135135 Ki = 5.0 nM 8.30
CHEMBL134304 Ki = 16.0 nM 7.80
CHEMBL1161079 Ki = 17.0 nM 7.77
CHEMBL423712 Ki = 20.0 nM 7.70
CHEMBL1161087 Ki = 22.0 nM 7.66
CHEMBL443546 Ki = 23.0 nM 7.64
CHEMBL275045 Ki = 23.0 nM 7.64
CHEMBL1161096 Ki = 28.0 nM 7.55
CHEMBL334767 Ki = 31.0 nM 7.51
CHEMBL1161088 Ki = 31.0 nM 7.51
CHEMBL3392290 Ki = 32.0 nM 7.50
CHEMBL10105 Ki = 46.0 nM 7.34
CHEMBL135676 Ki = 51.0 nM 7.29
CHEMBL1161120 Ki = 53.0 nM 7.28
CHEMBL341402 Ki = 56.0 nM 7.25
CHEMBL1161083 Ki = 57.0 nM 7.24
CHEMBL1161076 Ki = 63.0 nM 7.20
CHEMBL1161078 Ki = 65.0 nM 7.19
CHEMBL340268 Ki = 87.0 nM 7.06
CHEMBL135107 Ki = 90.0 nM 7.05
CHEMBL135938 Ki = 90.0 nM 7.05
CHEMBL416703 Ki = 120.0 nM 6.92
CHEMBL135129 Ki = 198.0 nM 6.70
CHEMBL439607 Ki = 302.0 nM 6.52
CHEMBL134951 Ki > 1000.0 nM -