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Assay Detail

CHEMBL672803

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

Functional
Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Pituitary gland cell
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor.
DeNinno MP, Schoenleber R, Perner RJ, Lijewski L, Asin KE, Britton DR, MacKenzie R, Kebabian JW.
J Med Chem (1991) 34 : 2561 -2569
PubMed 1652023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 5.84 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87734 1 6.72
CHEMBL86325 1 6.69
CHEMBL315849 1 6.54
CHEMBL431220 1 6.45
CHEMBL415080 1 6.45
CHEMBL85409 1 6.37
CHEMBL85689 1 6.12
CHEMBL420972 1 6.11
CHEMBL87958 1 5.54
CHEMBL83080 1 5.54
CHEMBL315468 1 5.41
CHEMBL2114209 1 5.29
CHEMBL420604 1 5.17
CHEMBL314459 1 5.15
CHEMBL86931 1 4.99
CHEMBL2115213 1 4.97
CHEMBL84557 1 -
CHEMBL315535 1 -
CHEMBL24077 (R)-SKF-38393 1 -
CHEMBL313304 1 -
CHEMBL87897 1 -
CHEMBL82899 1 -
CHEMBL315005 1 -
CHEMBL315750 1 -
CHEMBL85552 1 -
CHEMBL313530 1 -
CHEMBL86576 1 -
CHEMBL315516 1 -
CHEMBL86669 1 -
CHEMBL419680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87734 EC50 = 192.0 nM 6.72
CHEMBL86325 EC50 = 204.0 nM 6.69
CHEMBL315849 EC50 = 286.0 nM 6.54
CHEMBL431220 EC50 = 359.0 nM 6.45
CHEMBL415080 EC50 = 358.0 nM 6.45
CHEMBL85409 EC50 = 427.0 nM 6.37
CHEMBL85689 EC50 = 760.0 nM 6.12
CHEMBL420972 EC50 = 782.0 nM 6.11
CHEMBL87958 EC50 = 2850.0 nM 5.54
CHEMBL83080 EC50 = 2850.0 nM 5.54
CHEMBL315468 EC50 = 3910.0 nM 5.41
CHEMBL2114209 EC50 = 5130.0 nM 5.29
CHEMBL420604 EC50 = 6680.0 nM 5.17
CHEMBL314459 EC50 = 7030.0 nM 5.15
CHEMBL86931 EC50 = 10200.0 nM 4.99
CHEMBL2115213 EC50 = 10800.0 nM 4.97
CHEMBL420788 EC50 > 10000.0 nM -
CHEMBL87910 EC50 > 10000.0 nM -
CHEMBL87172 EC50 > 10000.0 nM -
CHEMBL84983 EC50 > 10000.0 nM -
CHEMBL419680 EC50 > 10000.0 nM -
CHEMBL86669 EC50 > 10000.0 nM -
CHEMBL315516 EC50 > 10000.0 nM -
CHEMBL86576 EC50 > 10000.0 nM -
CHEMBL313530 EC50 > 10000.0 nM -
CHEMBL85552 EC50 > 10000.0 nM -
CHEMBL315750 EC50 > 10000.0 nM -
CHEMBL315005 EC50 > 1000.0 nM -
CHEMBL82899 EC50 > 10000.0 nM -
CHEMBL87897 EC50 > 10000.0 nM -
CHEMBL313304 EC50 > 10000.0 nM -
CHEMBL24077 (R)-SKF-38393 EC50 > 10000.0 nM -
CHEMBL315535 EC50 > 10000.0 nM -
CHEMBL84557 EC50 > 10000.0 nM -