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Assay Detail

CHEMBL1944112

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

Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.
Peprah K, Zhu XY, Eyunni SV, Setola V, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2012) 20 : 1291 -1297
PubMed 22245230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.05 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1940402 1 8.82
CHEMBL1940420 1 8.74
CHEMBL1940404 1 8.62
CHEMBL1940418 1 8.46
CHEMBL1940417 1 8.38
CHEMBL1940414 1 8.35
CHEMBL1940413 1 8.25
CHEMBL1940419 1 8.24
CHEMBL1940415 1 8.21
CHEMBL140872 1 8.19
CHEMBL1940411 1 8.16
CHEMBL1940412 1 8.13
CHEMBL1940408 1 8.11
CHEMBL1940409 1 8.06
CHEMBL1940406 1 8.02
CHEMBL1940416 1 7.68
CHEMBL1940407 1 7.46
CHEMBL1940405 1 7.41
CHEMBL1940410 1 7.05
CHEMBL1940403 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1940402 Ki = 1.5 nM 8.82
CHEMBL1940420 Ki = 1.8 nM 8.74
CHEMBL1940404 Ki = 2.4 nM 8.62
CHEMBL1940418 Ki = 3.5 nM 8.46
CHEMBL1940417 Ki = 4.2 nM 8.38
CHEMBL1940414 Ki = 4.5 nM 8.35
CHEMBL1940413 Ki = 5.6 nM 8.25
CHEMBL1940419 Ki = 5.7 nM 8.24
CHEMBL1940415 Ki = 6.2 nM 8.21
CHEMBL140872 Ki = 6.5 nM 8.19
CHEMBL1940411 Ki = 6.9 nM 8.16
CHEMBL1940412 Ki = 7.4 nM 8.13
CHEMBL1940408 Ki = 7.8 nM 8.11
CHEMBL1940409 Ki = 8.7 nM 8.06
CHEMBL1940406 Ki = 9.5 nM 8.02
CHEMBL1940416 Ki = 21.0 nM 7.68
CHEMBL1940407 Ki = 35.0 nM 7.46
CHEMBL1940405 Ki = 39.0 nM 7.41
CHEMBL1940410 Ki = 89.0 nM 7.05
CHEMBL1940403 Ki = 247.8 nM 6.61