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Assay Detail

CHEMBL885886

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

Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
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 Intermediate

Target

D(1A) dopamine receptor (CHEMBL2056)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dopamine/serotonin receptor ligands. Part 15: Oxygenation of the benz-indolo-azecine LE 300 leads to novel subnanomolar dopamine D1/D5 antagonists.
Enzensperger C, Kilian S, Ackermann M, Koch A, Kelch K, Lehmann J.
Bioorg Med Chem Lett (2007) 17 : 1399 -1402
PubMed 17188870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.58 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201170 1 9.41
CHEMBL245570 1 9.25
CHEMBL396560 1 9.09
CHEMBL441618 1 8.72
CHEMBL245764 1 8.70
CHEMBL245571 1 8.43
CHEMBL201525 1 8.35
CHEMBL396561 1 7.72
CHEMBL380330 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201170 Ki = 0.39 nM 9.41
CHEMBL245570 Ki = 0.56 nM 9.25
CHEMBL396560 Ki = 0.82 nM 9.09
CHEMBL441618 Ki = 1.9 nM 8.72
CHEMBL245764 Ki = 2.0 nM 8.70
CHEMBL245571 Ki = 3.7 nM 8.43
CHEMBL201525 Ki = 4.5 nM 8.35
CHEMBL396561 Ki = 19.0 nM 7.72
CHEMBL380330 Ki = 28.5 nM 7.54