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Assay Detail

CHEMBL616088

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

Binding
Binding affinity was determined against 5-hydroxytryptamine 1A receptor using [3H]WB-4101
48
Total Activities
48
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

Piperazinylalkyl heterocycles as potential antipsychotic agents.
Scott MK, Baxter EW, Bennett DJ, Boyd RE, Blum PS, Codd EE, Kukla MJ, Malloy E, Maryanoff BE, Maryanoff CA.
J Med Chem (1995) 38 : 4198 -4210
PubMed 7473547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 8.00 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161097 1 10.15
CHEMBL1161065 1 9.60
CHEMBL544373 1 9.39
CHEMBL544371 1 9.20
CHEMBL1161068 1 9.08
CHEMBL1161055 1 8.85
CHEMBL1161061 1 8.82
CHEMBL10085 MAZAPERTINE 2.0 1 8.77
CHEMBL133765 1 8.72
CHEMBL1161063 1 8.72
CHEMBL1161052 1 8.64
CHEMBL542483 1 8.60
CHEMBL552830 1 8.51
CHEMBL538280 1 8.49
CHEMBL428175 RWJ-25730 1 8.38
CHEMBL1161071 1 8.38
CHEMBL1161064 1 8.35
CHEMBL1161059 1 8.34
CHEMBL1161074 1 8.33
CHEMBL49 BUSPIRONE 4.0 1 8.30
CHEMBL1161067 1 8.24
CHEMBL1161069 1 8.15
CHEMBL1161073 1 8.03
CHEMBL124285 1 8.00
CHEMBL1161045 1 7.96
CHEMBL1161075 1 7.96
CHEMBL1161051 1 7.92
CHEMBL1161094 1 7.92
CHEMBL1161044 1 7.80
CHEMBL1161057 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161097 Ki = 0.07 nM 10.15
CHEMBL1161065 Ki = 0.25 nM 9.60
CHEMBL544373 Ki = 0.41 nM 9.39
CHEMBL544371 Ki = 0.63 nM 9.20
CHEMBL1161068 Ki = 0.84 nM 9.08
CHEMBL1161055 Ki = 1.4 nM 8.85
CHEMBL1161061 Ki = 1.5 nM 8.82
CHEMBL10085 MAZAPERTINE Ki = 1.7 nM 8.77
CHEMBL133765 Ki = 1.9 nM 8.72
CHEMBL1161063 Ki = 1.9 nM 8.72
CHEMBL1161052 Ki = 2.3 nM 8.64
CHEMBL542483 Ki = 2.5 nM 8.60
CHEMBL552830 Ki = 3.1 nM 8.51
CHEMBL538280 Ki = 3.2 nM 8.49
CHEMBL1161071 Ki = 4.2 nM 8.38
CHEMBL428175 RWJ-25730 Ki = 4.2 nM 8.38
CHEMBL1161064 Ki = 4.5 nM 8.35
CHEMBL1161059 Ki = 4.6 nM 8.34
CHEMBL1161074 Ki = 4.7 nM 8.33
CHEMBL49 BUSPIRONE Ki = 5.0 nM 8.30
CHEMBL1161067 Ki = 5.7 nM 8.24
CHEMBL1161069 Ki = 7.1 nM 8.15
CHEMBL1161073 Ki = 9.4 nM 8.03
CHEMBL124285 Ki = 10.0 nM 8.00
CHEMBL1161045 Ki = 11.0 nM 7.96
CHEMBL1161075 Ki = 11.0 nM 7.96
CHEMBL1161051 Ki = 12.0 nM 7.92
CHEMBL1161094 Ki = 12.0 nM 7.92
CHEMBL1161044 Ki = 16.0 nM 7.80
CHEMBL1161057 Ki = 18.0 nM 7.75
CHEMBL1161072 Ki = 21.0 nM 7.68
CHEMBL1161046 Ki = 25.0 nM 7.60
CHEMBL1161095 Ki = 27.0 nM 7.57
CHEMBL1161060 Ki = 29.0 nM 7.54
CHEMBL1161043 Ki = 32.0 nM 7.50
CHEMBL1161070 Ki = 38.0 nM 7.42
CHEMBL1161066 Ki = 39.0 nM 7.41
CHEMBL42 CLOZAPINE Ki = 39.0 nM 7.41
CHEMBL1161056 Ki = 39.0 nM 7.41
CHEMBL1161049 Ki = 48.0 nM 7.32
CHEMBL1161054 Ki = 51.0 nM 7.29
CHEMBL1161048 Ki = 57.0 nM 7.24
CHEMBL538529 Ki = 94.0 nM 7.03
CHEMBL133880 Ki = 120.0 nM 6.92
CHEMBL1161050 Ki = 248.0 nM 6.61
CHEMBL54 HALOPERIDOL Ki = 401.0 nM 6.40
CHEMBL553555 Ki = 829.0 nM 6.08
CHEMBL334889 Ki = 1000.0 nM 6.00