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Assay Detail

CHEMBL670102

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

Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-(substituted-phenyl) piperazines: antagonists with high binding and functional selectivity for dopamine D4 receptors
Boyfield I, Coldwell MC, Hadley MS, Healy MA, Johns A, Nash DJ, Riley GJ, Scott EE, Smith SA, Stemp G, Wilson K
Bioorg Med Chem Lett (1996) 6 : 1227 -1232
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.37 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21168 1 8.30
CHEMBL283353 1 8.10
CHEMBL20655 1 8.10
CHEMBL20725 1 8.10
CHEMBL20367 1 8.00
CHEMBL20493 1 7.90
CHEMBL21008 1 7.90
CHEMBL20444 1 7.90
CHEMBL21011 1 7.80
CHEMBL20251 1 7.80
CHEMBL21119 1 7.70
CHEMBL282008 1 7.60
CHEMBL20996 1 7.50
CHEMBL277669 1 7.50
CHEMBL21059 1 7.30
CHEMBL20854 1 7.20
CHEMBL20204 1 7.20
CHEMBL283142 1 7.10
CHEMBL20729 1 7.00
CHEMBL20114 1 6.90
CHEMBL278288 1 6.90
CHEMBL277937 1 6.90
CHEMBL21205 1 6.80
CHEMBL423287 1 6.70
CHEMBL20819 1 6.50
CHEMBL21035 1 6.50
CHEMBL21252 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21168 Ki = 5.012 nM 8.30
CHEMBL283353 Ki = 7.943 nM 8.10
CHEMBL20655 Ki = 7.943 nM 8.10
CHEMBL20725 Ki = 7.943 nM 8.10
CHEMBL20367 Ki = 10.0 nM 8.00
CHEMBL20493 Ki = 12.59 nM 7.90
CHEMBL21008 Ki = 12.59 nM 7.90
CHEMBL20444 Ki = 12.59 nM 7.90
CHEMBL21011 Ki = 15.85 nM 7.80
CHEMBL20251 Ki = 15.85 nM 7.80
CHEMBL21119 Ki = 19.95 nM 7.70
CHEMBL282008 Ki = 25.12 nM 7.60
CHEMBL20996 Ki = 31.62 nM 7.50
CHEMBL277669 Ki = 31.62 nM 7.50
CHEMBL21059 Ki = 50.12 nM 7.30
CHEMBL20854 Ki = 63.1 nM 7.20
CHEMBL20204 Ki = 63.1 nM 7.20
CHEMBL283142 Ki = 79.43 nM 7.10
CHEMBL20729 Ki = 100.0 nM 7.00
CHEMBL20114 Ki = 125.89 nM 6.90
CHEMBL278288 Ki = 125.89 nM 6.90
CHEMBL277937 Ki = 125.89 nM 6.90
CHEMBL21205 Ki = 158.49 nM 6.80
CHEMBL423287 Ki = 199.53 nM 6.70
CHEMBL20819 Ki = 316.23 nM 6.50
CHEMBL21035 Ki = 316.23 nM 6.50
CHEMBL21252 Ki = 1258.93 nM 5.90