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Assay Detail

CHEMBL616273

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

Binding
In vitro binding affinity against 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT in human CYP3A4 assay
22
Total Activities
22
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 (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.
Tandon M, O'Donnell MM, Porte A, Vensel D, Yang D, Palma R, Beresford A, Ashwell MA.
Bioorg Med Chem Lett (2004) 14 : 1709 -1712
PubMed 15026055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.03 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27429 1 8.70
CHEMBL297099 1 8.40
CHEMBL47497 1 7.92
CHEMBL296254 1 7.82
CHEMBL49 BUSPIRONE 4.0 1 7.60
CHEMBL46075 1 7.34
CHEMBL281720 1 7.22
CHEMBL44837 1 7.20
CHEMBL49432 1 7.19
CHEMBL46095 1 7.16
CHEMBL49586 1 7.06
CHEMBL47419 1 7.00
CHEMBL284092 GEPIRONE 4.0 1 6.94
CHEMBL49575 1 6.69
CHEMBL49489 1 6.68
CHEMBL47628 1 6.36
CHEMBL45853 1 6.34
CHEMBL44992 1 6.15
CHEMBL297306 1 6.08
CHEMBL299406 1 6.03
CHEMBL49950 1 5.84
CHEMBL297543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27429 IC50 = 2.0 nM 8.70
CHEMBL297099 IC50 = 4.0 nM 8.40
CHEMBL47497 IC50 = 12.0 nM 7.92
CHEMBL296254 IC50 = 15.0 nM 7.82
CHEMBL49 BUSPIRONE IC50 = 25.0 nM 7.60
CHEMBL46075 IC50 = 46.0 nM 7.34
CHEMBL281720 IC50 = 60.0 nM 7.22
CHEMBL44837 IC50 = 63.0 nM 7.20
CHEMBL49432 IC50 = 64.0 nM 7.19
CHEMBL46095 IC50 = 69.0 nM 7.16
CHEMBL49586 IC50 = 87.0 nM 7.06
CHEMBL47419 IC50 = 99.0 nM 7.00
CHEMBL284092 GEPIRONE IC50 = 114.0 nM 6.94
CHEMBL49575 IC50 = 205.0 nM 6.69
CHEMBL49489 IC50 = 210.0 nM 6.68
CHEMBL47628 IC50 = 440.0 nM 6.36
CHEMBL45853 IC50 = 460.0 nM 6.34
CHEMBL44992 IC50 = 710.0 nM 6.15
CHEMBL297306 IC50 = 840.0 nM 6.08
CHEMBL299406 IC50 = 930.0 nM 6.03
CHEMBL49950 IC50 = 1460.0 nM 5.84
CHEMBL297543 IC50 > 1000.0 nM -