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Assay Detail

CHEMBL961819

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

Functional
Antagonist activity at human D2 like receptor expressed in HEK293 cells assessed as inhibition of quinpirole-stimulated mitogenesis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

N-(4-(4-(2,3-dichloro- or 2-methoxyphenyl)piperazin-1-yl)butyl)heterobiarylcarboxamides with functionalized linking chains as high affinity and enantioselective D3 receptor antagonists.
Newman AH, Grundt P, Cyriac G, Deschamps JR, Taylor M, Kumar R, Ho D, Luedtke RR.
J Med Chem (2009) 52 : 2559 -2570
PubMed 19331412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.74 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124444 1 8.09
CHEMBL424294 1 7.67
CHEMBL1627324 1 7.64
CHEMBL1627304 1 7.24
CHEMBL59725 1 7.02
CHEMBL366904 1 6.96
CHEMBL139926 1 6.93
CHEMBL1627320 1 6.83
CHEMBL1627309 1 6.79
CHEMBL182379 1 6.77
CHEMBL1627323 1 6.76
CHEMBL175734 1 6.59
CHEMBL1627311 1 6.57
CHEMBL1627321 1 6.47
CHEMBL1627319 1 6.39
CHEMBL1627308 1 6.37
CHEMBL184383 1 5.99
CHEMBL1627310 1 5.67
CHEMBL1627305 1 5.36
CHEMBL1627307 1 -
CHEMBL1627306 1 -
CHEMBL1627314 1 -
CHEMBL1627315 1 -
CHEMBL1627316 1 -
CHEMBL1627317 1 -
CHEMBL1627318 1 -
CHEMBL1627312 1 -
CHEMBL1627313 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124444 IC50 = 8.2 nM 8.09
CHEMBL424294 IC50 = 21.4 nM 7.67
CHEMBL1627324 IC50 = 23.0 nM 7.64
CHEMBL1627304 IC50 = 58.0 nM 7.24
CHEMBL59725 IC50 = 94.7 nM 7.02
CHEMBL366904 IC50 = 111.0 nM 6.96
CHEMBL139926 IC50 = 118.0 nM 6.93
CHEMBL1627320 IC50 = 146.1 nM 6.83
CHEMBL1627309 IC50 = 162.0 nM 6.79
CHEMBL182379 IC50 = 170.0 nM 6.77
CHEMBL1627323 IC50 = 175.0 nM 6.76
CHEMBL175734 IC50 = 254.0 nM 6.59
CHEMBL1627311 IC50 = 270.0 nM 6.57
CHEMBL1627321 IC50 = 340.0 nM 6.47
CHEMBL1627319 IC50 = 405.0 nM 6.39
CHEMBL1627308 IC50 = 427.0 nM 6.37
CHEMBL184383 IC50 = 1030.0 nM 5.99
CHEMBL1627310 IC50 = 2160.0 nM 5.67
CHEMBL1627305 IC50 = 4370.0 nM 5.36
CHEMBL1627307 IC50 - -
CHEMBL1627306 IC50 - -
CHEMBL1627314 IC50 - -
CHEMBL1627315 IC50 - -
CHEMBL1627316 IC50 - -
CHEMBL1627317 IC50 - -
CHEMBL1627318 IC50 - -
CHEMBL1627312 IC50 - -
CHEMBL1627313 IC50 - -