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Assay Detail

CHEMBL873170

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

Binding
In vitro for binding affinity against Alpha-2 adrenergic receptor by radioligand [3H]clonidine in rat
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adrenergic receptor alpha-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Effect of ring size or an additional heteroatom on the potency and selectivity of bicyclic benzylamine-type inhibitors of phenylethanolamine N-methyltransferase.
Grunewald GL, Dahanukar VH, Ching P, Criscione KR.
J Med Chem (1996) 39 : 3539 -3546
PubMed 8784452 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.54 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE 1 6.46
CHEMBL294079 1 6.28
CHEMBL118475 1 6.09
CHEMBL60434 1 6.08
CHEMBL323692 1 5.58
CHEMBL118420 1 5.39
CHEMBL333343 1 5.34
CHEMBL293023 1 5.21
CHEMBL118310 1 4.96
CHEMBL116945 1 4.80
CHEMBL522 BENZYLAMINE 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14346 1,2,3,4-TETRAHYDROISOQUINOLINE Ki = 350.0 nM 6.46
CHEMBL294079 Ki = 520.0 nM 6.28
CHEMBL118475 Ki = 820.0 nM 6.09
CHEMBL60434 Ki = 840.0 nM 6.08
CHEMBL323692 Ki = 2600.0 nM 5.58
CHEMBL118420 Ki = 4100.0 nM 5.39
CHEMBL333343 Ki = 4600.0 nM 5.34
CHEMBL293023 Ki = 6200.0 nM 5.21
CHEMBL118310 Ki = 11000.0 nM 4.96
CHEMBL116945 Ki = 16000.0 nM 4.80
CHEMBL522 BENZYLAMINE Ki = 20000.0 nM 4.70