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Assay Detail

CHEMBL5050784

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

Binding
Inhibition of PLD1 (unknown origin) expressed in human HEK cells by immunoprecipitation assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phospholipase D1 (CHEMBL2536)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
May-Dracka TL, Gao F, Hopkins BT, Hronowski X, Chen T, Chodaparambil JV, Metrick CM, Cullivan M, Enyedy I, Kaliszczak M, Kankel MW, Marx I, Michell-Robinson MA, Murugan P, Kumar PR, Rooney M, Schuman E, Sen A, Wang T, Ye T, Peterson EA.
ACS Med Chem Lett (2022) 13 : 665 -673
PubMed 35450377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.82 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5085284 1 7.66
CHEMBL5078848 1 7.48
CHEMBL5092677 1 7.40
CHEMBL5078394 1 7.37
CHEMBL5085809 1 7.36
CHEMBL4446255 1 7.31
CHEMBL5092708 1 7.18
CHEMBL5088048 1 7.17
CHEMBL5083605 1 7.15
CHEMBL5086717 1 7.12
CHEMBL5074314 1 7.00
CHEMBL5092706 1 6.96
CHEMBL5075520 1 6.92
CHEMBL5076666 1 6.89
CHEMBL5080858 1 6.85
CHEMBL5086297 1 6.77
CHEMBL5080277 1 6.70
CHEMBL5080618 1 6.55
CHEMBL5080871 1 6.50
CHEMBL5081973 1 6.44
CHEMBL5093394 1 6.42
CHEMBL5090919 1 6.31
CHEMBL5085765 1 6.01
CHEMBL5094742 1 5.92
CHEMBL5092637 1 5.03
CHEMBL5083676 1 -
CHEMBL5087594 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5085284 IC50 = 22.0 nM 7.66
CHEMBL5078848 IC50 = 33.0 nM 7.48
CHEMBL5092677 IC50 = 40.0 nM 7.40
CHEMBL5078394 IC50 = 43.0 nM 7.37
CHEMBL5085809 IC50 = 44.0 nM 7.36
CHEMBL4446255 IC50 = 49.0 nM 7.31
CHEMBL5092708 IC50 = 66.0 nM 7.18
CHEMBL5088048 IC50 = 68.0 nM 7.17
CHEMBL5083605 IC50 = 71.0 nM 7.15
CHEMBL5086717 IC50 = 76.0 nM 7.12
CHEMBL5074314 IC50 = 100.0 nM 7.00
CHEMBL5092706 IC50 = 110.0 nM 6.96
CHEMBL5075520 IC50 = 120.0 nM 6.92
CHEMBL5076666 IC50 = 130.0 nM 6.89
CHEMBL5080858 IC50 = 140.0 nM 6.85
CHEMBL5086297 IC50 = 170.0 nM 6.77
CHEMBL5080277 IC50 = 200.0 nM 6.70
CHEMBL5080618 IC50 = 280.0 nM 6.55
CHEMBL5080871 IC50 = 320.0 nM 6.50
CHEMBL5081973 IC50 = 360.0 nM 6.44
CHEMBL5093394 IC50 = 380.0 nM 6.42
CHEMBL5090919 IC50 = 490.0 nM 6.31
CHEMBL5085765 IC50 = 970.0 nM 6.01
CHEMBL5094742 IC50 = 1200.0 nM 5.92
CHEMBL5092637 IC50 = 9300.0 nM 5.03
CHEMBL5083676 IC50 > 10000.0 nM -
CHEMBL5087594 IC50 > 10000.0 nM -