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Assay Detail

CHEMBL615581

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

Binding
Affinity towards 5-hydroxytryptamine 1A receptor in membranes from bovine hippocampus using [3H]OH-DPAT
21
Total Activities
21
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

Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
Taverne T, Diouf O, Depreux P, Poupaert JH, Lesieur D, Guardiola-Lemaître B, Renard P, Rettori MC, Caignard DH, Pfeiffer B.
J Med Chem (1998) 41 : 2010 -2018
PubMed 9622542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.47 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64878 1 9.70
CHEMBL60447 1 9.70
CHEMBL304438 1 9.70
CHEMBL60885 1 9.52
CHEMBL64610 1 9.22
CHEMBL60047 1 9.15
CHEMBL64167 1 9.15
CHEMBL61869 1 9.15
CHEMBL59823 1 9.10
CHEMBL61819 1 9.10
CHEMBL418499 1 9.00
CHEMBL61818 1 8.70
CHEMBL293923 1 8.70
CHEMBL59637 1 8.52
CHEMBL294730 1 8.52
CHEMBL292935 1 7.96
CHEMBL60318 1 7.40
CHEMBL64845 1 7.37
CHEMBL42 CLOZAPINE 4.0 1 6.82
CHEMBL54 HALOPERIDOL 4.0 1 5.82
CHEMBL59741 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64878 IC50 = 0.2 nM 9.70
CHEMBL60447 IC50 = 0.2 nM 9.70
CHEMBL304438 IC50 = 0.2 nM 9.70
CHEMBL60885 IC50 = 0.3 nM 9.52
CHEMBL64610 IC50 = 0.6 nM 9.22
CHEMBL60047 IC50 = 0.7 nM 9.15
CHEMBL64167 IC50 = 0.7 nM 9.15
CHEMBL61869 IC50 = 0.7 nM 9.15
CHEMBL59823 IC50 = 0.8 nM 9.10
CHEMBL61819 IC50 = 0.8 nM 9.10
CHEMBL418499 IC50 = 1.0 nM 9.00
CHEMBL61818 IC50 = 2.0 nM 8.70
CHEMBL293923 IC50 = 2.0 nM 8.70
CHEMBL59637 IC50 = 3.0 nM 8.52
CHEMBL294730 IC50 = 3.0 nM 8.52
CHEMBL292935 IC50 = 11.0 nM 7.96
CHEMBL60318 IC50 = 40.0 nM 7.40
CHEMBL64845 IC50 = 43.0 nM 7.37
CHEMBL42 CLOZAPINE IC50 = 150.0 nM 6.82
CHEMBL54 HALOPERIDOL IC50 = 1500.0 nM 5.82
CHEMBL59741 IC50 = 3000.0 nM 5.52