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Assay Detail

CHEMBL616109

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

Binding
In vitro ability to displace [3H]8-hydroxy-2-(di-n-propylamino) tetralin binding from 5-hydroxytryptamine 1A receptor site in rat brain hippocampus
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of central nervous system agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor site.
Mokrosz JL, Pietrasiewicz M, Duszyńska B, Cegła MT.
J Med Chem (1992) 35 : 2369 -2374
PubMed 1535661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.69 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279906 1 8.57
CHEMBL8412 IPSAPIRONE 2.0 1 8.47
CHEMBL27378 1 8.26
CHEMBL26650 1 7.74
CHEMBL284092 GEPIRONE 4.0 1 7.50
CHEMBL27192 1 6.91
CHEMBL281918 1 6.90
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 6.84
CHEMBL26737 1 6.82
CHEMBL307204 1 6.80
CHEMBL27298 1 6.78
CHEMBL26540 1 6.70
CHEMBL413527 1 6.66
CHEMBL76783 1 6.60
CHEMBL78740 1 5.14
CHEMBL282367 1 4.83
CHEMBL26782 1 4.51
CHEMBL284887 1 4.31
CHEMBL26904 1 -
CHEMBL418386 1 -
CHEMBL27099 1 -
CHEMBL77181 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279906 Ki = 2.67 nM 8.57
CHEMBL8412 IPSAPIRONE Ki = 3.4 nM 8.47
CHEMBL27378 Ki = 5.54 nM 8.26
CHEMBL26650 Ki = 18.4 nM 7.74
CHEMBL284092 GEPIRONE Ki = 31.8 nM 7.50
CHEMBL27192 Ki = 122.0 nM 6.91
CHEMBL281918 Ki = 127.0 nM 6.90
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 143.0 nM 6.84
CHEMBL26737 Ki = 152.0 nM 6.82
CHEMBL307204 Ki = 159.0 nM 6.80
CHEMBL27298 Ki = 166.0 nM 6.78
CHEMBL26540 Ki = 202.0 nM 6.70
CHEMBL413527 Ki = 220.0 nM 6.66
CHEMBL76783 Ki = 251.0 nM 6.60
CHEMBL78740 Ki = 7220.0 nM 5.14
CHEMBL282367 Ki = 14800.0 nM 4.83
CHEMBL26782 Ki = 30800.0 nM 4.51
CHEMBL284887 Ki = 49000.0 nM 4.31
CHEMBL26904 Ki > 100000.0 nM -
CHEMBL418386 Ki > 100000.0 nM -
CHEMBL27099 Ki > 100000.0 nM -
CHEMBL77181 Ki > 100000.0 nM -