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Assay Detail

CHEMBL648820

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

Binding
Displacement of [3H]prazosin from Alpha-1 adrenergic receptor
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.
Bioorg Med Chem Lett (2003) 13 : 829 -832
PubMed 12617901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.93 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166599 2 6.37
CHEMBL167004 1 6.31
CHEMBL166935 1 6.17
CHEMBL169469 1 6.14
CHEMBL166697 1 6.14
CHEMBL169695 1 6.00
CHEMBL166991 1 5.92
CHEMBL354482 1 5.77
CHEMBL299294 1 5.64
CHEMBL168496 1 5.50
CHEMBL170552 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166599 Ki = 430.0 nM 6.37
CHEMBL167004 Ki = 490.0 nM 6.31
CHEMBL166935 Ki = 670.0 nM 6.17
CHEMBL169469 Ki = 730.0 nM 6.14
CHEMBL166697 Ki = 730.0 nM 6.14
CHEMBL169695 Ki = 1000.0 nM 6.00
CHEMBL166991 Ki = 1200.0 nM 5.92
CHEMBL354482 Ki = 1700.0 nM 5.77
CHEMBL166599 Ki = 1800.0 nM 5.75
CHEMBL299294 Ki = 2300.0 nM 5.64
CHEMBL168496 Ki = 3200.0 nM 5.50
CHEMBL170552 Ki = 3300.0 nM 5.48