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Assay Detail

CHEMBL5361632

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

Binding
Inhibition of recombinant rat P2X7 receptor by FLIPR assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 7 (CHEMBL2496)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

From lead to clinic: A review of the structural design of P2X7R antagonists.
Zhang R, Li N, Zhao M, Tang M, Jiang X, Cai X, Ye N, Su K, Peng J, Zhang X, Wu W, Ye H.
Eur J Med Chem (2023) 251 : 115234 -115234
PubMed 36893624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.22 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3697516 1 8.60
CHEMBL3697521 1 8.36
CHEMBL3697509 1 8.35
CHEMBL3697511 1 8.09
CHEMBL3697517 1 6.74
CHEMBL3697540 1 5.40
CHEMBL3697551 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3697516 IC50 = 2.5 nM 8.60
CHEMBL3697521 IC50 = 4.4 nM 8.36
CHEMBL3697509 IC50 = 4.5 nM 8.35
CHEMBL3697511 IC50 = 8.1 nM 8.09
CHEMBL3697517 IC50 = 180.3 nM 6.74
CHEMBL3697540 IC50 = 3980.0 nM 5.40
CHEMBL3697551 IC50 = 10000.0 nM 5.00