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Assay Detail

CHEMBL961809

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

Binding
Displacement of [125]IABN from human cloned D2 like receptor expressed in HEK293 cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 31 6.81 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424294 1 7.67
CHEMBL68740 1 7.61
CHEMBL1627321 1 7.55
CHEMBL124444 1 7.44
CHEMBL125916 1 7.43
CHEMBL139926 1 7.35
CHEMBL1627309 1 7.33
CHEMBL1627322 1 7.28
CHEMBL1627304 1 7.22
CHEMBL59725 1 7.19
CHEMBL366904 1 7.12
CHEMBL1627323 1 7.12
CHEMBL182379 1 7.11
CHEMBL1627324 1 7.10
CHEMBL175734 1 6.83
CHEMBL184383 1 6.81
CHEMBL1627311 1 6.61
CHEMBL1627308 1 6.60
CHEMBL1627310 1 6.53
CHEMBL1627320 1 6.47
CHEMBL1627315 1 6.41
CHEMBL1627319 1 6.37
CHEMBL1627306 1 6.36
CHEMBL1627314 1 6.31
CHEMBL1627305 1 6.30
CHEMBL1627317 1 6.29
CHEMBL1627313 1 6.28
CHEMBL1627318 1 6.24
CHEMBL1627316 1 6.21
CHEMBL1627307 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424294 Ki = 21.5 nM 7.67
CHEMBL68740 Ki = 24.8 nM 7.61
CHEMBL1627321 Ki = 28.4 nM 7.55
CHEMBL124444 Ki = 36.5 nM 7.44
CHEMBL125916 Ki = 37.4 nM 7.43
CHEMBL139926 Ki = 44.8 nM 7.35
CHEMBL1627309 Ki = 47.1 nM 7.33
CHEMBL1627322 Ki = 52.5 nM 7.28
CHEMBL1627304 Ki = 60.0 nM 7.22
CHEMBL59725 Ki = 64.7 nM 7.19
CHEMBL366904 Ki = 76.5 nM 7.12
CHEMBL1627323 Ki = 76.4 nM 7.12
CHEMBL182379 Ki = 77.0 nM 7.11
CHEMBL1627324 Ki = 78.8 nM 7.10
CHEMBL175734 Ki = 149.0 nM 6.83
CHEMBL184383 Ki = 154.0 nM 6.81
CHEMBL1627311 Ki = 244.0 nM 6.61
CHEMBL1627308 Ki = 249.0 nM 6.60
CHEMBL1627310 Ki = 293.0 nM 6.53
CHEMBL1627320 Ki = 337.0 nM 6.47
CHEMBL1627315 Ki = 390.0 nM 6.41
CHEMBL1627319 Ki = 430.0 nM 6.37
CHEMBL1627306 Ki = 433.0 nM 6.36
CHEMBL1627314 Ki = 489.0 nM 6.31
CHEMBL1627305 Ki = 502.0 nM 6.30
CHEMBL1627317 Ki = 507.0 nM 6.29
CHEMBL1627313 Ki = 520.0 nM 6.28
CHEMBL1627318 Ki = 581.0 nM 6.24
CHEMBL1627316 Ki = 622.0 nM 6.21
CHEMBL1627307 Ki = 715.0 nM 6.15
CHEMBL1627312 Ki = 1060.0 nM 5.97