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Assay Detail

CHEMBL615940

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

Binding
In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex.
32
Total Activities
32
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

New (2-methoxyphenyl)piperazine derivatives as 5-HT1A receptor ligands with reduced alpha 1-adrenergic activity. Synthesis and structure-affinity relationships.
Orjales A, Alonso-Cires L, Labeaga L, Corcóstegui R.
J Med Chem (1995) 38 : 1273 -1277
PubMed 7731013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 8.35 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23847 1 9.92
CHEMBL22482 1 9.64
CHEMBL25654 1 9.62
CHEMBL23946 1 9.57
CHEMBL22600 1 9.42
CHEMBL23877 1 9.20
CHEMBL23505 1 9.13
CHEMBL56 8-OH-DPAT 1 8.93
CHEMBL282453 1 8.92
CHEMBL8618 NAN-190 1 8.90
CHEMBL22427 1 8.81
CHEMBL23904 1 8.73
CHEMBL282012 1 8.66
CHEMBL22601 1 8.64
CHEMBL23449 1 8.63
CHEMBL22871 1 8.51
CHEMBL23315 1 8.48
CHEMBL23266 1 8.42
CHEMBL23905 1 8.33
CHEMBL276953 1 8.17
CHEMBL280426 1 7.94
CHEMBL278604 1 7.90
CHEMBL49 BUSPIRONE 4.0 1 7.81
CHEMBL22872 1 7.76
CHEMBL278799 1 7.69
CHEMBL23912 1 7.60
CHEMBL23530 1 7.49
CHEMBL23817 1 7.49
CHEMBL442065 1 7.25
CHEMBL23264 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23847 Ki = 0.12 nM 9.92
CHEMBL22482 Ki = 0.23 nM 9.64
CHEMBL25654 Ki = 0.24 nM 9.62
CHEMBL23946 Ki = 0.27 nM 9.57
CHEMBL22600 Ki = 0.38 nM 9.42
CHEMBL23877 Ki = 0.63 nM 9.20
CHEMBL23505 Ki = 0.74 nM 9.13
CHEMBL56 8-OH-DPAT Ki = 1.18 nM 8.93
CHEMBL282453 Ki = 1.19 nM 8.92
CHEMBL8618 NAN-190 Ki = 1.26 nM 8.90
CHEMBL22427 Ki = 1.53 nM 8.81
CHEMBL23904 Ki = 1.88 nM 8.73
CHEMBL282012 Ki = 2.2 nM 8.66
CHEMBL22601 Ki = 2.29 nM 8.64
CHEMBL23449 Ki = 2.34 nM 8.63
CHEMBL22871 Ki = 3.09 nM 8.51
CHEMBL23315 Ki = 3.34 nM 8.48
CHEMBL23266 Ki = 3.8 nM 8.42
CHEMBL23905 Ki = 4.68 nM 8.33
CHEMBL276953 Ki = 6.83 nM 8.17
CHEMBL280426 Ki = 11.6 nM 7.94
CHEMBL278604 Ki = 12.5 nM 7.90
CHEMBL49 BUSPIRONE Ki = 15.4 nM 7.81
CHEMBL22872 Ki = 17.5 nM 7.76
CHEMBL278799 Ki = 20.3 nM 7.69
CHEMBL23912 Ki = 25.2 nM 7.60
CHEMBL23530 Ki = 32.13 nM 7.49
CHEMBL23817 Ki = 32.3 nM 7.49
CHEMBL442065 Ki = 55.71 nM 7.25
CHEMBL23264 Ki = 201.0 nM 6.70
CHEMBL24113 Ki = 321.0 nM 6.49
CHEMBL26447 Ki = 362.0 nM 6.44