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Assay Detail

CHEMBL982103

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

Binding
Displacement of [3H]SCH23390 from human cloned dopamine D2L receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Dopamine/serotonin receptor ligands. Part 17: a cross-target SAR approach: affinities of azecine-styled ligands for 5-HT(2A) versus D1 and D2 receptors.
Enzensperger C, Görnemann T, Pertz HH, Lehmann J.
Bioorg Med Chem Lett (2008) 18 : 3809 -3813
PubMed 18534847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.42 8.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203637 1 8.45
CHEMBL380330 1 7.89
CHEMBL216258 1 7.87
CHEMBL201170 1 7.76
CHEMBL389357 1 7.61
CHEMBL441618 1 7.38
CHEMBL231070 1 7.38
CHEMBL245570 1 7.36
CHEMBL201525 1 7.23
CHEMBL508399 1 7.11
CHEMBL276778 1 7.06
CHEMBL216439 1 6.94
CHEMBL459871 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203637 Ki = 3.548 nM 8.45
CHEMBL380330 Ki = 12.88 nM 7.89
CHEMBL216258 Ki = 13.49 nM 7.87
CHEMBL201170 Ki = 17.38 nM 7.76
CHEMBL389357 Ki = 24.55 nM 7.61
CHEMBL441618 Ki = 41.69 nM 7.38
CHEMBL231070 Ki = 41.69 nM 7.38
CHEMBL245570 Ki = 43.65 nM 7.36
CHEMBL201525 Ki = 58.88 nM 7.23
CHEMBL508399 Ki = 77.62 nM 7.11
CHEMBL276778 Ki = 86.7 nM 7.06
CHEMBL216439 Ki = 114.82 nM 6.94
CHEMBL459871 Ki = 389.05 nM 6.41