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Assay Detail

CHEMBL5250271

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

Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL ↗
102
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.
Tolentino KT, Mashinson V, Sharma MK, Chhonker YS, Murry DJ, Hopkins CR.
Eur J Med Chem (2022) 244 : 114840 -114840
PubMed 36283180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 102 6.59 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267014 L-745870 — 2 9.26
CHEMBL3793438 — — 2 8.48
CHEMBL3905761 — — 2 8.46
CHEMBL3793910 — — 2 8.30
CHEMBL5282085 — — 2 7.55
CHEMBL5270824 — — 2 7.04
CHEMBL5190239 — — 2 7.02
CHEMBL5172055 — — 2 6.92
CHEMBL5195130 — — 2 6.88
CHEMBL5182191 — — 2 6.87
CHEMBL5196102 — — 2 6.87
CHEMBL5170670 — — 2 6.83
CHEMBL5206427 — — 2 6.80
CHEMBL5189986 — — 2 6.78
CHEMBL5270836 — — 2 6.77
CHEMBL5201507 — — 2 6.77
CHEMBL5179198 — — 2 6.76
CHEMBL5175548 — — 2 6.70
CHEMBL5207898 — — 2 6.69
CHEMBL5193761 — — 2 6.68
CHEMBL5174731 — — 2 6.67
CHEMBL5187429 — — 2 6.62
CHEMBL5274285 — — 2 6.57
CHEMBL5209344 — — 2 6.56
CHEMBL5179459 — — 2 6.52
CHEMBL5204764 — — 2 6.52
CHEMBL5171398 — — 2 6.50
CHEMBL5280960 — — 2 6.50
CHEMBL5171772 — — 2 6.49
CHEMBL5208124 — — 2 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267014 L-745870 Ki = 0.5495 nM 9.26
CHEMBL267014 L-745870 Ki = 0.6 nM 9.22
CHEMBL3793438 — Ki = 3.311 nM 8.48
CHEMBL3793438 — Ki = 3.3 nM 8.48
CHEMBL3905761 — Ki = 3.5 nM 8.46
CHEMBL3905761 — Ki = 3.548 nM 8.45
CHEMBL3793910 — Ki = 5.0 nM 8.30
CHEMBL3793910 — Ki = 5.012 nM 8.30
CHEMBL5282085 — Ki = 28.0 nM 7.55
CHEMBL5282085 — Ki = 28.18 nM 7.55
CHEMBL5270824 — Ki = 91.2 nM 7.04
CHEMBL5270824 — Ki = 91.0 nM 7.04
CHEMBL5190239 — Ki = 95.5 nM 7.02
CHEMBL5190239 — Ki = 96.0 nM 7.02
CHEMBL5172055 — Ki = 120.23 nM 6.92
CHEMBL5172055 — Ki = 121.0 nM 6.92
CHEMBL5195130 — Ki = 131.83 nM 6.88
CHEMBL5182191 — Ki = 134.9 nM 6.87
CHEMBL5196102 — Ki = 134.9 nM 6.87
CHEMBL5196102 — Ki = 134.0 nM 6.87
CHEMBL5182191 — Ki = 135.0 nM 6.87
CHEMBL5170670 — Ki = 149.0 nM 6.83
CHEMBL5170670 — Ki = 147.91 nM 6.83
CHEMBL5206427 — Ki = 158.49 nM 6.80
CHEMBL5206427 — Ki = 158.0 nM 6.80
CHEMBL5189986 — Ki = 165.96 nM 6.78
CHEMBL5189986 — Ki = 165.0 nM 6.78
CHEMBL5201507 — Ki = 170.0 nM 6.77
CHEMBL5270836 — Ki = 169.82 nM 6.77
CHEMBL5270836 — Ki = 169.0 nM 6.77
CHEMBL5201507 — Ki = 169.82 nM 6.77
CHEMBL5179198 — Ki = 173.78 nM 6.76
CHEMBL5179198 — Ki = 175.0 nM 6.76
CHEMBL5175548 — Ki = 201.0 nM 6.70
CHEMBL5175548 — Ki = 199.53 nM 6.70
CHEMBL5207898 — Ki = 204.17 nM 6.69
CHEMBL5207898 — Ki = 206.0 nM 6.69
CHEMBL5193761 — Ki = 208.93 nM 6.68
CHEMBL5195130 — Ki = 208.0 nM 6.68
CHEMBL5193761 — Ki = 211.0 nM 6.68
CHEMBL5174731 — Ki = 213.8 nM 6.67
CHEMBL5174731 — Ki = 215.0 nM 6.67
CHEMBL5187429 — Ki = 241.0 nM 6.62
CHEMBL5187429 — Ki = 239.88 nM 6.62
CHEMBL5274285 — Ki = 269.15 nM 6.57
CHEMBL5274285 — Ki = 268.0 nM 6.57
CHEMBL5209344 — Ki = 275.42 nM 6.56
CHEMBL5209344 — Ki = 276.0 nM 6.56
CHEMBL5179459 — Ki = 302.0 nM 6.52
CHEMBL5204764 — Ki = 299.0 nM 6.52