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Assay Detail

CHEMBL646863

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

Binding
Affinity for alpha-1 adrenergic receptor in rat was determined by [3H]- prazosin binding assay
7
Total Activities
7
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 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Zhou ZL, Cai SX, Whittemore ER, Konkoy CS, Espitia SA, Tran M, Rock DM, Coughenour LL, Hawkinson JE, Boxer PA, Bigge CF, Wise LD, Weber E, Woodward RM, Keana JF.
J Med Chem (1999) 42 : 2993 -3000
PubMed 10425109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.81 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL 1 6.66
CHEMBL54778 1 6.33
CHEMBL102659 1 6.09
CHEMBL449704 1 5.80
CHEMBL103472 1 5.75
CHEMBL28564 ELIPRODIL 2.0 1 5.48
CHEMBL317229 1 4.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49623 (R,S)-IFENPRODIL IC50 = 220.0 nM 6.66
CHEMBL54778 IC50 = 470.0 nM 6.33
CHEMBL102659 IC50 = 820.0 nM 6.09
CHEMBL449704 IC50 = 1600.0 nM 5.80
CHEMBL103472 IC50 = 1800.0 nM 5.75
CHEMBL28564 ELIPRODIL IC50 = 3300.0 nM 5.48
CHEMBL317229 IC50 = 27000.0 nM 4.57