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Assay Detail

CHEMBL1274011

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

Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(4) dopamine receptor (CHEMBL3361)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.
Lacivita E, De Giorgio P, Lee IT, Rodeheaver SI, Weiss BA, Fracasso C, Caccia S, Berardi F, Perrone R, Zhang MR, Maeda J, Higuchi M, Suhara T, Schetz JA, Leopoldo M.
J Med Chem (2010) 53 : 7344 -7355
PubMed 20873719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.41 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1270323 1 9.47
CHEMBL1270423 1 9.03
CHEMBL1270121 1 8.82
CHEMBL1270227 1 8.75
CHEMBL1270013 1 8.71
CHEMBL1270322 1 8.58
CHEMBL1270516 1 8.54
CHEMBL93403 1 8.30
CHEMBL156845 1 8.04
CHEMBL345111 1 7.95
CHEMBL1270422 1 7.49
CHEMBL1270120 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1270323 Ki = 0.34 nM 9.47
CHEMBL1270423 Ki = 0.93 nM 9.03
CHEMBL1270121 Ki = 1.52 nM 8.82
CHEMBL1270227 Ki = 1.76 nM 8.75
CHEMBL1270013 Ki = 1.93 nM 8.71
CHEMBL1270322 Ki = 2.64 nM 8.58
CHEMBL1270516 Ki = 2.92 nM 8.54
CHEMBL93403 Ki = 4.97 nM 8.30
CHEMBL156845 Ki = 9.21 nM 8.04
CHEMBL345111 Ki = 11.29 nM 7.95
CHEMBL1270422 Ki = 32.71 nM 7.49
CHEMBL1270120 Ki = 63.95 nM 7.19