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Assay Detail

CHEMBL616586

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor by displacing [3H]WB-4101 from rat hippocampus
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyrrole mannich bases as potential antipsychotic agents.
Scott MK, Martin GE, DiStefano DL, Fedde CL, Kukla MJ, Barrett DL, Baldy WJ, Elgin RJ, Kesslick JM, Mathiasen JR.
J Med Chem (1992) 35 : 552 -558
PubMed 1346653 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.97 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346168 1 8.77
CHEMBL153136 1 8.74
CHEMBL428175 RWJ-25730 1 8.48
CHEMBL49 BUSPIRONE 4.0 1 8.30
CHEMBL434512 1 8.27
CHEMBL9666 1 8.02
CHEMBL153490 1 7.76
CHEMBL347334 1 7.52
CHEMBL153451 1 7.46
CHEMBL422 TRIFLUOPERAZINE 4.0 1 6.39
CHEMBL267044 LEVOSULPIRIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346168 Ki = 1.7 nM 8.77
CHEMBL153136 Ki = 1.8 nM 8.74
CHEMBL428175 RWJ-25730 Ki = 3.3 nM 8.48
CHEMBL49 BUSPIRONE Ki = 5.0 nM 8.30
CHEMBL434512 Ki = 5.4 nM 8.27
CHEMBL9666 Ki = 9.5 nM 8.02
CHEMBL153490 Ki = 17.2 nM 7.76
CHEMBL347334 Ki = 30.0 nM 7.52
CHEMBL153451 Ki = 34.3 nM 7.46
CHEMBL422 TRIFLUOPERAZINE Ki = 411.0 nM 6.39
CHEMBL267044 LEVOSULPIRIDE Ki > 1000.0 nM -