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Assay Detail

CHEMBL3100268

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Functional
Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR study of a novel series of dopamine receptor agonists.
Risgaard R, Jensen M, Jørgensen M, Bang-Andersen B, Christoffersen CT, Jensen KG, Kristensen JL, Püschl A.
Bioorg Med Chem (2014) 22 : 381 -392
PubMed 24296012 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.50 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099226 1 9.85
CHEMBL3098131 1 9.77
CHEMBL3099235 1 9.30
CHEMBL3099222 1 9.22
CHEMBL1303 ROTIGOTINE 4.0 1 9.15
CHEMBL3099225 1 9.10
CHEMBL3099231 1 9.00
CHEMBL3099227 1 8.96
CHEMBL3099230 1 8.82
CHEMBL3099234 1 8.77
CHEMBL3099236 1 8.68
CHEMBL3099239 1 8.46
CHEMBL3099224 1 8.40
CHEMBL3099232 1 7.89
CHEMBL3099228 1 7.75
CHEMBL3099223 1 7.60
CHEMBL3099233 1 7.48
CHEMBL59 DOPAMINE 4.0 1 7.44
CHEMBL3099229 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099226 EC50 = 0.14 nM 9.85
CHEMBL3098131 EC50 = 0.17 nM 9.77
CHEMBL3099235 EC50 = 0.5 nM 9.30
CHEMBL3099222 EC50 = 0.6 nM 9.22
CHEMBL1303 ROTIGOTINE EC50 = 0.7 nM 9.15
CHEMBL3099225 EC50 = 0.8 nM 9.10
CHEMBL3099231 EC50 = 1.0 nM 9.00
CHEMBL3099227 EC50 = 1.1 nM 8.96
CHEMBL3099230 EC50 = 1.5 nM 8.82
CHEMBL3099234 EC50 = 1.7 nM 8.77
CHEMBL3099236 EC50 = 2.1 nM 8.68
CHEMBL3099239 EC50 = 3.5 nM 8.46
CHEMBL3099224 EC50 = 4.0 nM 8.40
CHEMBL3099232 EC50 = 13.0 nM 7.89
CHEMBL3099228 EC50 = 18.0 nM 7.75
CHEMBL3099223 EC50 = 25.0 nM 7.60
CHEMBL3099233 EC50 = 33.0 nM 7.48
CHEMBL59 DOPAMINE EC50 = 36.0 nM 7.44
CHEMBL3099229 EC50 = 1400.0 nM 5.85