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Assay Detail

CHEMBL615902

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

Binding
In vitro inhibition of [3H]8-OH-DPAT binding to rat 5-HT 1a receptors.
20
Total Activities
20
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

1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V.
J Med Chem (1999) 42 : 490 -496
PubMed 9986719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.21 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL322275 1 9.30
CHEMBL444590 1 9.27
CHEMBL26929 1 9.11
CHEMBL147659 1 8.89
CHEMBL144523 1 8.80
CHEMBL148288 1 8.64
CHEMBL147861 1 8.62
CHEMBL146942 1 8.60
CHEMBL147963 1 8.37
CHEMBL148186 1 8.35
CHEMBL148234 1 8.15
CHEMBL148397 1 8.15
CHEMBL108241 1 8.11
CHEMBL147371 1 8.00
CHEMBL107486 1 8.00
CHEMBL147692 1 7.47
CHEMBL28063 1 7.42
CHEMBL49 BUSPIRONE 4.0 1 7.30
CHEMBL435029 1 7.05
CHEMBL359245 1 6.50

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
CHEMBL147659 IC50 = 1.3 nM 8.89
CHEMBL144523 IC50 = 1.6 nM 8.80
CHEMBL148288 IC50 = 2.3 nM 8.64
CHEMBL147861 IC50 = 2.4 nM 8.62
CHEMBL146942 IC50 = 2.5 nM 8.60
CHEMBL147963 IC50 = 4.3 nM 8.37
CHEMBL148186 IC50 = 4.5 nM 8.35
CHEMBL148234 IC50 = 7.0 nM 8.15
CHEMBL148397 IC50 = 7.0 nM 8.15
CHEMBL108241 IC50 = 7.7 nM 8.11
CHEMBL147371 IC50 = 10.0 nM 8.00
CHEMBL107486 IC50 = 10.0 nM 8.00
CHEMBL147692 IC50 = 34.0 nM 7.47
CHEMBL28063 IC50 = 38.0 nM 7.42
CHEMBL49 BUSPIRONE IC50 = 50.0 nM 7.30
CHEMBL435029 IC50 = 89.0 nM 7.05
CHEMBL359245 IC50 = 320.0 nM 6.50