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Assay Detail

CHEMBL3108480

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

Binding
Antagonist activity at human P2X1 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 1 (CHEMBL2094)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbamazepine derivatives with P2X4 receptor-blocking activity.
Tian M, Abdelrahman A, Weinhausen S, Hinz S, Weyer S, Dosa S, El-Tayeb A, Müller CE.
Bioorg Med Chem (2014) 22 : 1077 -1088
PubMed 24411477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.70 5.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3103375 1 5.34
CHEMBL3103385 1 5.27
CHEMBL3103371 1 4.68
CHEMBL1483754 1 4.60
CHEMBL3103372 1 4.16
CHEMBL3103369 1 4.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3103375 IC50 = 4550.0 nM 5.34
CHEMBL3103385 IC50 = 5320.0 nM 5.27
CHEMBL3103371 IC50 = 20700.0 nM 4.68
CHEMBL1483754 IC50 = 25200.0 nM 4.60
CHEMBL3103372 IC50 = 68800.0 nM 4.16
CHEMBL3103369 IC50 = 69600.0 nM 4.16