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Assay Detail

CHEMBL616164

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

Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 5A (CHEMBL4655)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Derivatives of 2-arylcyclopropylamine: Synthesis and interactions with 5-HT1A receptors.
Appelberg U, Mohell N, Hacksell U
Bioorg Med Chem Lett (1996) 6 : 415 -420
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.82 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34653 1 8.59
CHEMBL37844 1 8.31
CHEMBL34652 1 7.77
CHEMBL132123 1 7.24
CHEMBL132019 1 6.73
CHEMBL134331 1 6.62
CHEMBL336124 1 6.51
CHEMBL133433 1 6.42
CHEMBL133935 1 6.41
CHEMBL423527 1 6.37
CHEMBL341373 1 6.30
CHEMBL334553 1 6.13
CHEMBL133020 1 6.12
CHEMBL135894 1 6.00
CHEMBL132580 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34653 Ki = 2.6 nM 8.59
CHEMBL37844 Ki = 4.9 nM 8.31
CHEMBL34652 Ki = 17.0 nM 7.77
CHEMBL132123 Ki = 58.0 nM 7.24
CHEMBL132019 Ki = 186.0 nM 6.73
CHEMBL134331 Ki = 239.0 nM 6.62
CHEMBL336124 Ki = 310.0 nM 6.51
CHEMBL133433 Ki = 379.0 nM 6.42
CHEMBL133935 Ki = 388.0 nM 6.41
CHEMBL423527 Ki = 431.0 nM 6.37
CHEMBL341373 Ki = 506.0 nM 6.30
CHEMBL334553 Ki = 736.0 nM 6.13
CHEMBL133020 Ki = 752.0 nM 6.12
CHEMBL135894 Ki = 998.0 nM 6.00
CHEMBL132580 Ki > 10000.0 nM -