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Assay Detail

CHEMBL3239709

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

Binding
Displacement of [3H]methylspiperone from human D2L receptor expressed in HEK cell membrane after 90 mins by scintillation counting analysis
15
Total Activities
15
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 Autocuration

Target

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

Publication

Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.
Xiao J, Free RB, Barnaeva E, Conroy JL, Doyle T, Miller B, Bryant-Genevier M, Taylor MK, Hu X, Dulcey AE, Southall N, Ferrer M, Titus S, Zheng W, Sibley DR, Marugan JJ.
J Med Chem (2014) 57 : 3450 -3463
PubMed 24666157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.17 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1200270 1 9.05
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL445102 1 8.12
CHEMBL3234537 1 7.64
CHEMBL3234536 1 7.05
CHEMBL3234544 1 7.00
CHEMBL3234237 JNJ-37822681 2.0 1 6.80
CHEMBL3234522 1 6.72
CHEMBL3234543 1 6.68
CHEMBL3234541 1 6.62
CHEMBL3234539 1 6.54
CHEMBL1503220 1 6.52
CHEMBL3234542 1 6.51
CHEMBL3234538 1 6.28
CHEMBL3234545 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1200270 Ki = 0.9 nM 9.05
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL445102 Ki = 7.5 nM 8.12
CHEMBL3234537 Ki = 23.0 nM 7.64
CHEMBL3234536 Ki = 90.0 nM 7.05
CHEMBL3234544 Ki = 100.0 nM 7.00
CHEMBL3234237 JNJ-37822681 Ki = 158.0 nM 6.80
CHEMBL3234522 Ki = 190.0 nM 6.72
CHEMBL3234543 Ki = 210.0 nM 6.68
CHEMBL3234541 Ki = 240.0 nM 6.62
CHEMBL3234539 Ki = 290.0 nM 6.54
CHEMBL1503220 Ki = 300.0 nM 6.52
CHEMBL3234542 Ki = 310.0 nM 6.51
CHEMBL3234538 Ki = 530.0 nM 6.28
CHEMBL3234545 Ki > 50000.0 nM -