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Assay Detail

CHEMBL3591120

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Functional
Agonist activity at recombinant human alpha2c adrenergic receptor expressed in CHOK1 cells co-expressing Gqi5 assessed as induction of cytoplasmic calcium mobilization measured for 40 secs by fluorometric analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Cell-based and virtual fragment screening for adrenergic α2C receptor agonists.
Szőllősi E, Bobok A, Kiss L, Vass M, Kurkó D, Kolok S, Visegrády A, Keserű GM.
Bioorg Med Chem (2015) 23 : 3991 -3999
PubMed 25648685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 4.96 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL761 NAPHAZOLINE 4.0 1 7.26
CHEMBL3588902 1 6.76
CHEMBL286080 SKF-38393 1 5.86
CHEMBL2087646 1 5.50
CHEMBL3588904 1 5.46
CHEMBL3588911 1 3.83
CHEMBL1327 1 3.47
CHEMBL3588905 1 3.32
CHEMBL3588909 1 3.20
CHEMBL3588907 1 -
CHEMBL3588906 1 -
CHEMBL598391 1 -
CHEMBL3588908 1 -
CHEMBL3588903 1 -
CHEMBL3588910 1 -
CHEMBL3590203 1 -
CHEMBL341473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL761 NAPHAZOLINE EC50 = 54.95 nM 7.26
CHEMBL3588902 EC50 = 173.78 nM 6.76
CHEMBL286080 SKF-38393 EC50 = 1380.38 nM 5.86
CHEMBL2087646 EC50 = 3162.28 nM 5.50
CHEMBL3588904 EC50 = 3467.37 nM 5.46
CHEMBL3588911 EC50 = 147910.84 nM 3.83
CHEMBL1327 EC50 = 338844.16 nM 3.47
CHEMBL3588905 EC50 = 478630.09 nM 3.32
CHEMBL3588909 EC50 = 630957.34 nM 3.20
CHEMBL3588907 EC50 > 501187.23 nM -
CHEMBL3588906 EC50 > 501187.23 nM -
CHEMBL598391 EC50 > 501187.23 nM -
CHEMBL3588908 EC50 > 501187.23 nM -
CHEMBL3588903 EC50 > 501187.23 nM -
CHEMBL3588910 EC50 > 501187.23 nM -
CHEMBL3590203 EC50 > 501187.23 nM -
CHEMBL341473 EC50 > 501187.23 nM -