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Assay Detail

CHEMBL4362018

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

Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 14 (CHEMBL4518)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and anti-inflammatory evaluation of 3-amide benzoic acid derivatives as novel P2Y<sub>14</sub> receptor antagonists.
Zhang Z, Hao K, Li H, Lu R, Liu C, Zhou M, Li B, Meng Z, Hu Q, Jiang C.
Eur J Med Chem (2019) 181 : 111564 -111564
PubMed 31376563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.46 8.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436879 1 8.75
CHEMBL1800685 PPTN 1 8.70
CHEMBL4577585 1 8.50
CHEMBL4538561 1 8.36
CHEMBL4455311 1 8.34
CHEMBL4458922 1 8.30
CHEMBL4526840 1 8.30
CHEMBL4544516 1 -
CHEMBL4444277 1 -
CHEMBL4585569 1 -
CHEMBL4568716 1 -
CHEMBL4459825 1 -
CHEMBL4548774 1 -
CHEMBL4450096 1 -
CHEMBL4475814 1 -
CHEMBL4449331 1 -
CHEMBL4541044 1 -
CHEMBL4471193 1 -
CHEMBL4588599 1 -
CHEMBL4444167 1 -
CHEMBL4483489 1 -
CHEMBL4474050 1 -
CHEMBL4445922 1 -
CHEMBL4443140 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436879 IC50 = 1.77 nM 8.75
CHEMBL1800685 PPTN IC50 = 1.98 nM 8.70
CHEMBL4577585 IC50 = 3.17 nM 8.50
CHEMBL4538561 IC50 = 4.35 nM 8.36
CHEMBL4455311 IC50 = 4.54 nM 8.34
CHEMBL4458922 IC50 = 4.95 nM 8.30
CHEMBL4526840 IC50 = 5.06 nM 8.30
CHEMBL4544516 IC50 - -
CHEMBL4444277 IC50 - -
CHEMBL4585569 IC50 - -
CHEMBL4568716 IC50 - -
CHEMBL4459825 IC50 - -
CHEMBL4548774 IC50 - -
CHEMBL4450096 IC50 - -
CHEMBL4475814 IC50 - -
CHEMBL4449331 IC50 - -
CHEMBL4541044 IC50 - -
CHEMBL4471193 IC50 - -
CHEMBL4588599 IC50 - -
CHEMBL4444167 IC50 - -
CHEMBL4483489 IC50 - -
CHEMBL4474050 IC50 - -
CHEMBL4445922 IC50 - -
CHEMBL4443140 IC50 - -