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Assay Detail

CHEMBL616308

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

Binding
Affinity against the 5-hydroxytryptamine receptor 1A using [3H]WB-4101.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
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 37 7.98 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423712 1 9.89
CHEMBL1161079 1 8.92
CHEMBL10105 1 8.80
CHEMBL10085 MAZAPERTINE 2.0 1 8.77
CHEMBL1161083 1 8.59
CHEMBL428175 RWJ-25730 1 8.48
CHEMBL1161126 1 8.43
CHEMBL134304 1 8.43
CHEMBL340268 1 8.39
CHEMBL135135 1 8.35
CHEMBL1161078 1 8.29
CHEMBL275045 1 8.23
CHEMBL439607 1 8.21
CHEMBL443546 1 8.11
CHEMBL1161119 1 8.10
CHEMBL1161076 1 8.07
CHEMBL1161120 1 8.04
CHEMBL135129 1 8.00
CHEMBL416703 1 8.00
CHEMBL135676 1 7.96
CHEMBL135938 1 7.92
CHEMBL334767 1 7.92
CHEMBL1161088 1 7.92
CHEMBL1161087 1 7.77
CHEMBL135377 1 7.72
CHEMBL1161096 1 7.70
CHEMBL135047 1 7.60
CHEMBL341402 1 7.60
CHEMBL135479 1 7.54
CHEMBL135246 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423712 Ki = 0.13 nM 9.89
CHEMBL1161079 Ki = 1.2 nM 8.92
CHEMBL10105 Ki = 1.6 nM 8.80
CHEMBL10085 MAZAPERTINE Ki = 1.7 nM 8.77
CHEMBL1161083 Ki = 2.6 nM 8.59
CHEMBL428175 RWJ-25730 Ki = 3.3 nM 8.48
CHEMBL1161126 Ki = 3.7 nM 8.43
CHEMBL134304 Ki = 3.7 nM 8.43
CHEMBL340268 Ki = 4.1 nM 8.39
CHEMBL135135 Ki = 4.5 nM 8.35
CHEMBL1161078 Ki = 5.1 nM 8.29
CHEMBL275045 Ki = 5.9 nM 8.23
CHEMBL439607 Ki = 6.2 nM 8.21
CHEMBL443546 Ki = 7.8 nM 8.11
CHEMBL1161119 Ki = 8.0 nM 8.10
CHEMBL1161076 Ki = 8.6 nM 8.07
CHEMBL1161120 Ki = 9.2 nM 8.04
CHEMBL416703 Ki = 10.0 nM 8.00
CHEMBL135129 Ki = 10.0 nM 8.00
CHEMBL135676 Ki = 11.0 nM 7.96
CHEMBL135938 Ki = 12.0 nM 7.92
CHEMBL334767 Ki = 12.0 nM 7.92
CHEMBL1161088 Ki = 12.0 nM 7.92
CHEMBL1161087 Ki = 17.0 nM 7.77
CHEMBL135377 Ki = 19.0 nM 7.72
CHEMBL1161096 Ki = 20.0 nM 7.70
CHEMBL341402 Ki = 25.0 nM 7.60
CHEMBL135047 Ki = 25.0 nM 7.60
CHEMBL135479 Ki = 29.0 nM 7.54
CHEMBL135246 Ki = 29.0 nM 7.54
CHEMBL3392290 Ki = 31.0 nM 7.51
CHEMBL1161058 Ki = 31.0 nM 7.51
CHEMBL42 CLOZAPINE Ki = 38.5 nM 7.42
CHEMBL135107 Ki = 39.0 nM 7.41
CHEMBL422989 Ki = 41.0 nM 7.39
CHEMBL54 HALOPERIDOL Ki = 401.0 nM 6.40
CHEMBL134951 Ki = 460.0 nM 6.34