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Assay Detail

CHEMBL872367

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor in rat brain using [3H]prazosin
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent 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 : 1759 -1762
PubMed 12729659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.94 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL 1 7.92
CHEMBL50872 1 6.37
CHEMBL48743 1 5.89
CHEMBL48915 1 5.82
CHEMBL46779 1 5.66
CHEMBL299294 1 5.64
CHEMBL50166 1 5.50
CHEMBL48366 1 5.42
CHEMBL51594 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL Ki = 12.0 nM 7.92
CHEMBL50872 Ki = 430.0 nM 6.37
CHEMBL48743 Ki = 1300.0 nM 5.89
CHEMBL48915 Ki = 1500.0 nM 5.82
CHEMBL46779 Ki = 2200.0 nM 5.66
CHEMBL299294 Ki = 2300.0 nM 5.64
CHEMBL50166 Ki = 3200.0 nM 5.50
CHEMBL48366 Ki = 3800.0 nM 5.42
CHEMBL51594 Ki = 5800.0 nM 5.24