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Assay Detail

CHEMBL910434

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

Binding
Displacement of [125I]7-OH-PIPAT from human D2L receptor expressed in HEK293 cell membrane
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Discovery of 3-methyl-N-(1-oxy-3',4',5',6'-tetrahydro-2'H-[2,4'-bipyridine]-1'-ylmethyl)benzamide (ABT-670), an orally bioavailable dopamine D4 agonist for the treatment of erectile dysfunction.
Patel MV, Kolasa T, Mortell K, Matulenko MA, Hakeem AA, Rohde JJ, Nelson SL, Cowart MD, Nakane M, Miller LN, Uchic ME, Terranova MA, El-Kouhen OF, Donnelly-Roberts DL, Namovic MT, Hollingsworth PR, Chang R, Martino BR, Wetter JM, Marsh KC, Martin R, Darbyshire JF, Gintant G, Hsieh GC, Moreland RB, Sullivan JP, Brioni JD, Stewart AO.
J Med Chem (2006) 49 : 7450 -7465
PubMed 17149874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.73 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53 APOMORPHINE 4.0 1 8.44
CHEMBL376092 1 7.57
CHEMBL220189 1 6.63
CHEMBL375596 1 5.54
CHEMBL216794 1 5.46
CHEMBL219185 1 -
CHEMBL219179 1 -
CHEMBL219261 1 -
CHEMBL219182 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53 APOMORPHINE Ki = 3.6 nM 8.44
CHEMBL376092 Ki = 27.0 nM 7.57
CHEMBL220189 Ki = 235.0 nM 6.63
CHEMBL375596 Ki = 2900.0 nM 5.54
CHEMBL216794 Ki = 3500.0 nM 5.46
CHEMBL219185 Ki > 10000.0 nM -
CHEMBL219179 Ki > 10000.0 nM -
CHEMBL219261 Ki > 10000.0 nM -
CHEMBL219182 Ki > 10000.0 nM -