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Assay Detail

CHEMBL615914

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

Binding
In vitro binding affinity measured on serotonin 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand.
31
Total Activities
31
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

High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
Perrone R, Berardi F, Colabufo NA, Leopoldo M, Tortorella V, Fiorentini F, Olgiati V, Ghiglieri A, Govoni S.
J Med Chem (1995) 38 : 942 -949
PubMed 7699710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.32 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26929 1 9.49
CHEMBL140406 1 9.46
CHEMBL322275 1 9.44
CHEMBL368477 1 9.41
CHEMBL173190 1 9.28
CHEMBL444590 1 9.24
CHEMBL174703 1 8.97
CHEMBL56 8-OH-DPAT 1 8.96
CHEMBL174083 1 8.95
CHEMBL175300 1 8.85
CHEMBL424125 1 8.82
CHEMBL366459 1 8.81
CHEMBL28209 1 8.76
CHEMBL174300 1 8.73
CHEMBL367435 1 8.70
CHEMBL171181 1 8.47
CHEMBL172556 1 8.23
CHEMBL108241 1 8.15
CHEMBL172161 1 8.06
CHEMBL172363 1 8.05
CHEMBL172601 1 8.03
CHEMBL49 BUSPIRONE 4.0 1 7.89
CHEMBL174554 1 7.89
CHEMBL148055 1 7.74
CHEMBL425134 1 7.39
CHEMBL171974 1 7.25
CHEMBL277302 1 7.20
CHEMBL367723 1 7.05
CHEMBL433972 1 6.86
CHEMBL176819 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26929 IC50 = 0.32 nM 9.49
CHEMBL140406 IC50 = 0.35 nM 9.46
CHEMBL322275 IC50 = 0.36 nM 9.44
CHEMBL368477 IC50 = 0.39 nM 9.41
CHEMBL173190 IC50 = 0.52 nM 9.28
CHEMBL444590 IC50 = 0.58 nM 9.24
CHEMBL174703 IC50 = 1.08 nM 8.97
CHEMBL56 8-OH-DPAT IC50 = 1.1 nM 8.96
CHEMBL174083 IC50 = 1.13 nM 8.95
CHEMBL175300 IC50 = 1.4 nM 8.85
CHEMBL424125 IC50 = 1.5 nM 8.82
CHEMBL366459 IC50 = 1.53 nM 8.81
CHEMBL28209 IC50 = 1.73 nM 8.76
CHEMBL174300 IC50 = 1.84 nM 8.73
CHEMBL367435 IC50 = 2.0 nM 8.70
CHEMBL171181 IC50 = 3.38 nM 8.47
CHEMBL172556 IC50 = 5.94 nM 8.23
CHEMBL108241 IC50 = 7.01 nM 8.15
CHEMBL172161 IC50 = 8.8 nM 8.06
CHEMBL172363 IC50 = 8.83 nM 8.05
CHEMBL172601 IC50 = 9.24 nM 8.03
CHEMBL49 BUSPIRONE IC50 = 12.8 nM 7.89
CHEMBL174554 IC50 = 13.0 nM 7.89
CHEMBL148055 IC50 = 18.3 nM 7.74
CHEMBL425134 IC50 = 40.3 nM 7.39
CHEMBL171974 IC50 = 55.9 nM 7.25
CHEMBL277302 IC50 = 63.6 nM 7.20
CHEMBL367723 IC50 = 88.4 nM 7.05
CHEMBL433972 IC50 = 138.0 nM 6.86
CHEMBL176819 IC50 = 146.0 nM 6.84
CHEMBL143110 IC50 = 147.0 nM 6.83