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Assay Detail

CHEMBL1680807

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

Functional
Antagonist activity against rat P2X2 receptor expressed in Xenopus laevis oocyte assessed as inhibition of alpha, beta-meATP-induced inward current by two-electrode voltage-clamp electrophysiology
ChEMBL ↗
65
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2X purinoceptor 2 (CHEMBL2135) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.
Baqi Y, Hausmann R, Rosefort C, Rettinger J, Schmalzing G, Müller CE.
J Med Chem (2011) 54 : 817 -830
PubMed 21207957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.95 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672104 — — 1 7.10
CHEMBL1672105 — — 1 7.07
CHEMBL271672 — — 1 7.00
CHEMBL496401 — — 1 6.93
CHEMBL1672106 — — 1 6.71
CHEMBL499580 — — 1 6.53
CHEMBL1672107 — — 1 6.52
CHEMBL509572 — — 1 6.24
CHEMBL496030 — — 1 6.23
CHEMBL1671995 — — 1 6.21
CHEMBL271688 — — 1 6.16
CHEMBL445413 — — 1 6.10
CHEMBL606414 — — 1 6.00
CHEMBL524064 — — 1 6.00
CHEMBL1672103 — — 1 6.00
CHEMBL1672102 — — 1 6.00
CHEMBL596982 — — 1 6.00
CHEMBL597591 — — 1 6.00
CHEMBL495796 — — 1 6.00
CHEMBL133576 ACID BLUE 129 — 1 6.00
CHEMBL498038 — — 1 6.00
CHEMBL495834 — — 1 6.00
CHEMBL521709 — — 1 6.00
CHEMBL522053 — — 1 6.00
CHEMBL524284 — — 1 6.00
CHEMBL499428 — — 1 6.00
CHEMBL604300 — — 1 6.00
CHEMBL597820 — — 1 6.00
CHEMBL256057 ACID BLUE 25 — 1 6.00
CHEMBL450832 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672104 — IC50 = 79.0 nM 7.10
CHEMBL1672105 — IC50 = 86.0 nM 7.07
CHEMBL271672 — IC50 = 100.0 nM 7.00
CHEMBL496401 — IC50 = 117.0 nM 6.93
CHEMBL1672106 — IC50 = 197.0 nM 6.71
CHEMBL499580 — IC50 = 293.0 nM 6.53
CHEMBL1672107 — IC50 = 300.0 nM 6.52
CHEMBL509572 — IC50 = 582.0 nM 6.24
CHEMBL496030 — IC50 = 588.0 nM 6.23
CHEMBL1671995 — IC50 = 623.0 nM 6.21
CHEMBL271688 — IC50 = 690.0 nM 6.16
CHEMBL445413 — IC50 = 800.0 nM 6.10
CHEMBL596982 — IC50 = 1000.0 nM 6.00
CHEMBL1672103 — IC50 = 1000.0 nM 6.00
CHEMBL499428 — IC50 = 1000.0 nM 6.00
CHEMBL598857 — IC50 = 1000.0 nM 6.00
CHEMBL256864 — IC50 = 1000.0 nM 6.00
CHEMBL404450 — IC50 = 1000.0 nM 6.00
CHEMBL606414 — IC50 = 1000.0 nM 6.00
CHEMBL402239 — IC50 = 1000.0 nM 6.00
CHEMBL256688 — IC50 = 1000.0 nM 6.00
CHEMBL522725 — IC50 = 1000.0 nM 6.00
CHEMBL403051 — IC50 = 1000.0 nM 6.00
CHEMBL597203 — IC50 = 1000.0 nM 6.00
CHEMBL604158 — IC50 = 1000.0 nM 6.00
CHEMBL1672098 — IC50 = 1000.0 nM 6.00
CHEMBL496022 — IC50 = 1000.0 nM 6.00
CHEMBL597591 — IC50 = 1000.0 nM 6.00
CHEMBL522053 — IC50 = 1000.0 nM 6.00
CHEMBL604300 — IC50 = 1000.0 nM 6.00
CHEMBL524284 — IC50 = 1000.0 nM 6.00
CHEMBL256057 ACID BLUE 25 IC50 = 1000.0 nM 6.00
CHEMBL597820 — IC50 = 1000.0 nM 6.00
CHEMBL450832 — IC50 = 1000.0 nM 6.00
CHEMBL524064 — IC50 = 1000.0 nM 6.00
CHEMBL521709 — IC50 = 1000.0 nM 6.00
CHEMBL495834 — IC50 = 1000.0 nM 6.00
CHEMBL498038 — IC50 = 1000.0 nM 6.00
CHEMBL133576 ACID BLUE 129 IC50 = 1000.0 nM 6.00
CHEMBL495796 — IC50 = 1000.0 nM 6.00
CHEMBL1672102 — IC50 = 1000.0 nM 6.00
CHEMBL131271 — IC50 = 1160.0 nM 5.94
CHEMBL401735 — IC50 = 1730.0 nM 5.76
CHEMBL257495 — IC50 = 2000.0 nM 5.70
CHEMBL477339 — IC50 = 4000.0 nM 5.40
CHEMBL1672108 TNP-ATP SODIUM IC50 = 4000.0 nM 5.40
CHEMBL223344 RB 2 IC50 = 4000.0 nM 5.40
CHEMBL265502 SURAMIN IC50 = 4000.0 nM 5.40
CHEMBL1672108 TNP-ATP SODIUM IC50 = 39810.72 nM 4.40
CHEMBL265502 SURAMIN IC50 = 39810.72 nM 4.40