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Assay Detail

CHEMBL615442

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

Binding
Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of bovine hippocampus.
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 2-substituted tetrahydro-3H-benz[e]indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants.
Romero AG, Leiby JA, McCall RB, Piercey MF, Smith MW, Han F.
J Med Chem (1993) 36 : 2066 -2074
PubMed 8101876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.60 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71920 U-92,016-A 1 10.00
CHEMBL1744088 1 9.70
CHEMBL1744035 1 9.40
CHEMBL1744037 1 9.22
CHEMBL1744036 1 8.80
CHEMBL1788190 1 8.72
CHEMBL1788192 1 8.57
CHEMBL1788324 1 8.55
CHEMBL49 BUSPIRONE 4.0 1 8.51
CHEMBL1744038 1 8.28
CHEMBL1744089 1 8.12
CHEMBL1788325 1 6.99
CHEMBL1788191 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71920 U-92,016-A Ki = 0.1 nM 10.00
CHEMBL1744088 Ki = 0.2 nM 9.70
CHEMBL1744035 Ki = 0.4 nM 9.40
CHEMBL1744037 Ki = 0.6 nM 9.22
CHEMBL1744036 Ki = 1.6 nM 8.80
CHEMBL1788190 Ki = 1.9 nM 8.72
CHEMBL1788192 Ki = 2.7 nM 8.57
CHEMBL1788324 Ki = 2.8 nM 8.55
CHEMBL49 BUSPIRONE Ki = 3.1 nM 8.51
CHEMBL1744038 Ki = 5.3 nM 8.28
CHEMBL1744089 Ki = 7.6 nM 8.12
CHEMBL1788325 Ki = 103.0 nM 6.99
CHEMBL1788191 Ki = 108.0 nM 6.97