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Assay Detail

CHEMBL3587537

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

Functional
Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay
24
Total Activities
12
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

Investigation of novel ropinirole analogues: synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands
Jorg M, Kaczor AA, Mak FS, Lee KCK, Poso A, Miller ND, Scammells PJ, Capuano B
Medchemcomm (2014) 5 : 891 -898
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 7.21 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3585370 2 8.41
CHEMBL3585371 2 8.21
CHEMBL3585372 2 7.85
CHEMBL3585369 2 7.66
CHEMBL3585368 2 7.55
CHEMBL3585367 2 7.38
CHEMBL155731 QUINELORANE 2.0 2 7.35
CHEMBL3585364 2 7.26
CHEMBL3585363 2 7.07
CHEMBL3585365 2 6.66
CHEMBL3585366 2 5.85
CHEMBL3585373 2 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3585370 EC50 = 3.9 nM 8.41
CHEMBL3585370 EC50 = 3.89 nM 8.41
CHEMBL3585371 EC50 = 6.166 nM 8.21
CHEMBL3585371 EC50 = 6.2 nM 8.21
CHEMBL3585372 EC50 = 14.13 nM 7.85
CHEMBL3585372 EC50 = 14.0 nM 7.85
CHEMBL3585369 EC50 = 22.0 nM 7.66
CHEMBL3585369 EC50 = 22.39 nM 7.65
CHEMBL3585368 EC50 = 28.18 nM 7.55
CHEMBL3585368 EC50 = 28.0 nM 7.55
CHEMBL3585367 EC50 = 41.69 nM 7.38
CHEMBL3585367 EC50 = 42.0 nM 7.38
CHEMBL155731 QUINELORANE EC50 = 45.0 nM 7.35
CHEMBL155731 QUINELORANE EC50 = 44.67 nM 7.35
CHEMBL3585364 EC50 = 55.0 nM 7.26
CHEMBL3585364 EC50 = 54.95 nM 7.26
CHEMBL3585363 EC50 = 85.0 nM 7.07
CHEMBL3585363 EC50 = 85.11 nM 7.07
CHEMBL3585365 EC50 = 219.0 nM 6.66
CHEMBL3585365 EC50 = 218.78 nM 6.66
CHEMBL3585366 EC50 = 1413.0 nM 5.85
CHEMBL3585366 EC50 = 1445.44 nM 5.84
CHEMBL3585373 EC50 = 4677.35 nM 5.33
CHEMBL3585373 EC50 = 4677.0 nM 5.33