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Assay Detail

CHEMBL615880

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor using receptor binding assay
26
Total Activities
26
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

Novel pyridazino[4,5-b][1,5]oxazepines and -thiazepines as 5-HT1A receptor ligands
Matyus P, Varga I, Zara E, Mezei A, Behr A, Simay A, Haider N, Boros S, Bakonyi A, Horvath E, Horvath K
Bioorg Med Chem Lett (1997) 7 : 2857 -2862
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.16 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49 BUSPIRONE 4.0 1 8.15
CHEMBL56 8-OH-DPAT 1 8.09
CHEMBL318857 1 8.04
CHEMBL316490 1 7.94
CHEMBL319937 1 7.75
CHEMBL95832 1 7.71
CHEMBL318260 1 7.49
CHEMBL95310 1 7.43
CHEMBL95837 1 7.35
CHEMBL95641 1 6.93
CHEMBL100260 1 6.87
CHEMBL318926 1 6.82
CHEMBL97711 1 6.79
CHEMBL318912 1 6.74
CHEMBL329283 1 6.64
CHEMBL97618 1 6.52
CHEMBL431096 1 6.51
CHEMBL99523 1 6.28
CHEMBL316929 1 6.00
CHEMBL319600 1 -
CHEMBL95981 1 -
CHEMBL99177 1 -
CHEMBL97198 1 -
CHEMBL95744 1 -
CHEMBL97623 1 -
CHEMBL95977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49 BUSPIRONE IC50 = 7.13 nM 8.15
CHEMBL56 8-OH-DPAT IC50 = 8.06 nM 8.09
CHEMBL318857 IC50 = 9.2 nM 8.04
CHEMBL316490 IC50 = 11.4 nM 7.94
CHEMBL319937 IC50 = 17.8 nM 7.75
CHEMBL95832 IC50 = 19.5 nM 7.71
CHEMBL318260 IC50 = 32.7 nM 7.49
CHEMBL95310 IC50 = 37.0 nM 7.43
CHEMBL95837 IC50 = 44.9 nM 7.35
CHEMBL95641 IC50 = 118.0 nM 6.93
CHEMBL100260 IC50 = 134.0 nM 6.87
CHEMBL318926 IC50 = 150.0 nM 6.82
CHEMBL97711 IC50 = 163.0 nM 6.79
CHEMBL318912 IC50 = 181.0 nM 6.74
CHEMBL329283 IC50 = 230.0 nM 6.64
CHEMBL97618 IC50 = 299.0 nM 6.52
CHEMBL431096 IC50 = 312.0 nM 6.51
CHEMBL99523 IC50 = 524.0 nM 6.28
CHEMBL316929 IC50 = 1003.0 nM 6.00
CHEMBL319600 IC50 > 1000.0 nM -
CHEMBL95981 IC50 > 1000.0 nM -
CHEMBL99177 IC50 > 1000.0 nM -
CHEMBL97198 IC50 > 1000.0 nM -
CHEMBL95744 IC50 > 1000.0 nM -
CHEMBL97623 IC50 > 1000.0 nM -
CHEMBL95977 IC50 > 1000.0 nM -