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Assay Detail

CHEMBL616108

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

Binding
Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand.
54
Total Activities
54
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

Synthesis and structure-activity relationships of a new model of arylpiperazines. 1. 2-[[4-(o-methoxyphenyl)piperazin-1-yl]methyl]-1, 3-dioxoperhydroimidazo[1,5-alpha]pyridine: a selective 5-HT1A receptor agonist.
López-Rodríguez ML, Rosado ML, Benhamú B, Morcillo MJ, Sanz AM, Orensanz L, Beneitez ME, Fuentes JA, Manzanares J.
J Med Chem (1996) 39 : 4439 -4450
PubMed 8893838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 7.38 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8618 NAN-190 1 9.22
CHEMBL46918 1 8.62
CHEMBL42706 1 8.42
CHEMBL43992 1 8.39
CHEMBL289873 1 8.36
CHEMBL42810 1 8.26
CHEMBL45253 1 8.24
CHEMBL42644 1 8.14
CHEMBL46881 1 8.06
CHEMBL417709 1 8.00
CHEMBL290039 1 7.95
CHEMBL290203 1 7.72
CHEMBL49 BUSPIRONE 4.0 1 7.69
CHEMBL43332 1 7.61
CHEMBL295168 1 7.50
CHEMBL46471 1 7.46
CHEMBL296713 1 7.34
CHEMBL44786 1 7.27
CHEMBL416984 1 7.25
CHEMBL296413 1 7.24
CHEMBL297844 1 7.24
CHEMBL297887 1 7.23
CHEMBL42396 1 7.18
CHEMBL9666 1 7.17
CHEMBL295244 1 7.11
CHEMBL42404 1 7.11
CHEMBL46470 1 7.07
CHEMBL46885 1 7.05
CHEMBL42654 1 7.00
CHEMBL430567 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8618 NAN-190 Ki = 0.6 nM 9.22
CHEMBL46918 Ki = 2.4 nM 8.62
CHEMBL42706 Ki = 3.8 nM 8.42
CHEMBL43992 Ki = 4.1 nM 8.39
CHEMBL289873 Ki = 4.4 nM 8.36
CHEMBL42810 Ki = 5.5 nM 8.26
CHEMBL45253 Ki = 5.7 nM 8.24
CHEMBL42644 Ki = 7.2 nM 8.14
CHEMBL46881 Ki = 8.8 nM 8.06
CHEMBL417709 Ki = 9.9 nM 8.00
CHEMBL290039 Ki = 11.3 nM 7.95
CHEMBL290203 Ki = 19.2 nM 7.72
CHEMBL49 BUSPIRONE Ki = 20.5 nM 7.69
CHEMBL43332 Ki = 24.8 nM 7.61
CHEMBL295168 Ki = 31.7 nM 7.50
CHEMBL46471 Ki = 34.9 nM 7.46
CHEMBL296713 Ki = 45.5 nM 7.34
CHEMBL44786 Ki = 53.6 nM 7.27
CHEMBL416984 Ki = 55.9 nM 7.25
CHEMBL296413 Ki = 57.9 nM 7.24
CHEMBL297844 Ki = 57.7 nM 7.24
CHEMBL297887 Ki = 58.4 nM 7.23
CHEMBL42396 Ki = 65.8 nM 7.18
CHEMBL9666 Ki = 68.0 nM 7.17
CHEMBL42404 Ki = 78.5 nM 7.11
CHEMBL295244 Ki = 78.6 nM 7.11
CHEMBL46470 Ki = 85.3 nM 7.07
CHEMBL46885 Ki = 89.9 nM 7.05
CHEMBL42654 Ki = 101.0 nM 7.00
CHEMBL430567 Ki = 120.0 nM 6.92
CHEMBL47200 Ki = 123.0 nM 6.91
CHEMBL46525 Ki = 128.0 nM 6.89
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 130.0 nM 6.89
CHEMBL41978 Ki = 154.0 nM 6.81
CHEMBL274866 Ki = 175.0 nM 6.76
CHEMBL46535 Ki = 234.0 nM 6.63
CHEMBL9434 PHENYLPIPERAZINE Ki = 380.0 nM 6.42
CHEMBL46802 Ki = 418.0 nM 6.38
CHEMBL46672 Ki = 444.0 nM 6.35
CHEMBL42881 Ki = 500.0 nM 6.30
CHEMBL45007 Ki = 598.0 nM 6.22
CHEMBL295527 Ki > 1000.0 nM -
CHEMBL296724 Ki > 1000.0 nM -
CHEMBL298286 Ki > 10000.0 nM -
CHEMBL46377 Ki > 10000.0 nM -
CHEMBL47040 Ki > 1000.0 nM -
CHEMBL432495 Ki > 10000.0 nM -
CHEMBL44876 Ki > 1000.0 nM -
CHEMBL291165 Ki > 1000.0 nM -
CHEMBL289784 Ki > 10000.0 nM -