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Assay Detail

CHEMBL648623

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

Binding
Inhibition of [3H]rauwolscine to CHO cells expressing the human Alpha-2C adrenergic receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-2C adrenergic receptor (CHEMBL1916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ruffolo RR, Bondinell W, Hieble JP.
J Med Chem (1995) 38 : 3681 -3716
PubMed 7562902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10347 RAUWOLSCINE 1 9.00
CHEMBL15245 YOHIMBINE 3.0 1 8.64
CHEMBL3559672 RAUWOLFIA SERPENTINA 4.0 1 8.30
CHEMBL123349 1 7.70
CHEMBL25467 1 7.68
CHEMBL122404 AKUAMMIGINE 1 7.55
CHEMBL123138 1 7.55
CHEMBL123448 1 7.46
CHEMBL114166 1 7.19
CHEMBL31410 CORYNANTHEINE 1 6.79
CHEMBL279436 1 6.78
CHEMBL284103 1 6.49
CHEMBL405355 NIGULDIPINE 2.0 1 6.43
CHEMBL3392247 1 6.25
CHEMBL5483012 1 5.88
CHEMBL3392246 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10347 RAUWOLSCINE Ki = 1.0 nM 9.00
CHEMBL15245 YOHIMBINE Ki = 2.3 nM 8.64
CHEMBL3559672 RAUWOLFIA SERPENTINA Ki = 5.0 nM 8.30
CHEMBL123349 Ki = 20.0 nM 7.70
CHEMBL25467 Ki = 21.0 nM 7.68
CHEMBL122404 AKUAMMIGINE Ki = 28.0 nM 7.55
CHEMBL123138 Ki = 28.0 nM 7.55
CHEMBL123448 Ki = 35.0 nM 7.46
CHEMBL114166 Ki = 64.0 nM 7.19
CHEMBL31410 CORYNANTHEINE Ki = 161.0 nM 6.79
CHEMBL279436 Ki = 165.0 nM 6.78
CHEMBL284103 Ki = 323.0 nM 6.49
CHEMBL405355 NIGULDIPINE Ki = 370.0 nM 6.43
CHEMBL3392247 Ki = 560.0 nM 6.25
CHEMBL5483012 Ki = 1320.0 nM 5.88
CHEMBL3392246 Ki = 1700.0 nM 5.77