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Assay Detail

CHEMBL615826

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

Binding
Binding affinity towards rat 5-hydroxytryptamine 1A receptor was evaluated using [3H]8-OH-DPAT as radioligand
19
Total Activities
19
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

Structure-activity relationship studies on the 5-HT(1A) receptor affinity of 1-phenyl-4-[omega-(alpha- or beta-tetralinyl)alkyl]piperazines. 4.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V, Fornaretto MG, Caccia C, McArthur RA.
J Med Chem (1996) 39 : 4928 -4934
PubMed 8960552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.97 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322275 1 9.30
CHEMBL444590 1 9.27
CHEMBL26929 1 9.11
CHEMBL56 8-OH-DPAT 1 8.68
CHEMBL144445 1 8.44
CHEMBL143728 1 8.43
CHEMBL147678 1 8.27
CHEMBL342518 1 8.14
CHEMBL357176 1 8.09
CHEMBL172601 1 8.03
CHEMBL341893 1 7.82
CHEMBL148055 1 7.74
CHEMBL147440 1 7.72
CHEMBL49 BUSPIRONE 4.0 1 7.52
CHEMBL343432 1 7.27
CHEMBL145432 1 7.25
CHEMBL144417 1 6.85
CHEMBL143110 1 6.83
CHEMBL147387 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL322275 IC50 = 0.5 nM 9.30
CHEMBL444590 IC50 = 0.54 nM 9.27
CHEMBL26929 IC50 = 0.77 nM 9.11
CHEMBL56 8-OH-DPAT IC50 = 2.1 nM 8.68
CHEMBL144445 IC50 = 3.6 nM 8.44
CHEMBL143728 IC50 = 3.7 nM 8.43
CHEMBL147678 IC50 = 5.4 nM 8.27
CHEMBL342518 IC50 = 7.3 nM 8.14
CHEMBL357176 IC50 = 8.2 nM 8.09
CHEMBL172601 IC50 = 9.24 nM 8.03
CHEMBL341893 IC50 = 15.0 nM 7.82
CHEMBL148055 IC50 = 18.3 nM 7.74
CHEMBL147440 IC50 = 19.0 nM 7.72
CHEMBL49 BUSPIRONE IC50 = 30.0 nM 7.52
CHEMBL343432 IC50 = 54.0 nM 7.27
CHEMBL145432 IC50 = 56.0 nM 7.25
CHEMBL144417 IC50 = 140.0 nM 6.85
CHEMBL143110 IC50 = 147.0 nM 6.83
CHEMBL147387 IC50 = 191.0 nM 6.72