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Assay Detail

CHEMBL942047

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

Functional
Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Pituitary gland cell
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
Blagg J, Allerton CM, Batchelor DV, Baxter AD, Burring DJ, Carr CL, Cook AS, Nichols CL, Phipps J, Sanderson VG, Verrier H, Wong S.
Bioorg Med Chem Lett (2007) 17 : 6691 -6696
PubMed 17976986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 7.24 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155731 QUINELORANE 2.0 1 8.70
CHEMBL53 APOMORPHINE 4.0 1 7.70
CHEMBL301265 PRAMIPEXOLE 4.0 1 7.57
CHEMBL589 ROPINIROLE 4.0 1 7.08
CHEMBL401328 1 5.14
CHEMBL250636 1 -
CHEMBL398694 1 -
CHEMBL399967 1 -
CHEMBL250829 1 -
CHEMBL250830 1 -
CHEMBL400987 1 -
CHEMBL250831 1 -
CHEMBL251023 1 -
CHEMBL400988 1 -
CHEMBL251215 1 -
CHEMBL398480 1 -
CHEMBL251216 1 -
CHEMBL250635 1 -
CHEMBL250634 1 -
CHEMBL400766 1 -
CHEMBL398696 1 -
CHEMBL101480 1 -
CHEMBL105646 1 -
CHEMBL250632 1 -
CHEMBL250403 1 -
CHEMBL250002 1 -
CHEMBL248595 1 -
CHEMBL401126 1 -
CHEMBL250003 1 -
CHEMBL401125 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155731 QUINELORANE EC50 = 2.0 nM 8.70
CHEMBL53 APOMORPHINE EC50 = 20.0 nM 7.70
CHEMBL301265 PRAMIPEXOLE EC50 = 27.0 nM 7.57
CHEMBL589 ROPINIROLE EC50 = 83.0 nM 7.08
CHEMBL401328 EC50 = 7200.0 nM 5.14
CHEMBL250636 EC50 > 10000.0 nM -
CHEMBL102463 EC50 > 10000.0 nM -
CHEMBL399967 EC50 - -
CHEMBL250829 EC50 - -
CHEMBL250830 EC50 - -
CHEMBL400987 EC50 > 1000.0 nM -
CHEMBL250831 EC50 > 1000.0 nM -
CHEMBL251023 EC50 - -
CHEMBL400988 EC50 > 10000.0 nM -
CHEMBL251215 EC50 > 30000.0 nM -
CHEMBL398480 EC50 > 100000.0 nM -
CHEMBL251216 EC50 > 10000.0 nM -
CHEMBL398694 EC50 > 10000.0 nM -
CHEMBL250635 EC50 - -
CHEMBL250634 EC50 > 10000.0 nM -
CHEMBL400766 EC50 > 10000.0 nM -
CHEMBL398696 EC50 > 1000.0 nM -
CHEMBL101480 EC50 > 10000.0 nM -
CHEMBL105646 EC50 > 10000.0 nM -
CHEMBL250632 EC50 > 10000.0 nM -
CHEMBL250403 EC50 > 10000.0 nM -
CHEMBL250002 EC50 > 10000.0 nM -
CHEMBL248595 EC50 > 10000.0 nM -
CHEMBL401126 EC50 > 10000.0 nM -
CHEMBL250003 EC50 > 10000.0 nM -
CHEMBL401125 EC50 > 10000.0 nM -