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Assay Detail

CHEMBL932853

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Functional
Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay
ChEMBL ↗
38
Total Activities
38
Compounds Tested
2
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 7 (CHEMBL2496) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Florjancic AS, Peddi S, Perez-Medrano A, Li B, Namovic MT, Grayson G, Donnelly-Roberts DL, Jarvis MF, Carroll WA.
Bioorg Med Chem Lett (2008) 18 : 2089 -2092
PubMed 18272366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.44 7.92
pIC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271462 — — 1 7.92
CHEMBL401822 — — 1 7.59
CHEMBL257045 — — 1 7.55
CHEMBL255614 — — 1 7.45
CHEMBL402132 — — 1 7.44
CHEMBL403222 — — 1 7.40
CHEMBL402411 — — 1 7.34
CHEMBL258111 — — 1 6.89
CHEMBL271030 — — 1 6.87
CHEMBL257897 — — 1 6.86
CHEMBL401531 — — 1 6.80
CHEMBL257523 — — 1 6.75
CHEMBL402133 — — 1 6.70
CHEMBL245754 — — 1 6.68
CHEMBL271679 — — 1 6.68
CHEMBL410039 — — 1 6.67
CHEMBL270678 — — 1 6.62
CHEMBL270679 — — 1 6.54
CHEMBL403763 — — 1 6.54
CHEMBL430223 — — 1 6.53
CHEMBL377219 — — 1 6.51
CHEMBL256883 — — 1 6.31
CHEMBL272933 — — 1 6.20
CHEMBL402412 — — 1 6.15
CHEMBL271464 — — 1 5.99
CHEMBL404091 — — 1 5.95
CHEMBL270421 — — 1 5.88
CHEMBL403907 — — 1 5.86
CHEMBL255638 — — 1 5.69
CHEMBL270019 — — 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271462 — IC50 = 12.02 nM 7.92
CHEMBL401822 — IC50 = 25.7 nM 7.59
CHEMBL257045 — IC50 = 28.18 nM 7.55
CHEMBL255614 — IC50 = 35.48 nM 7.45
CHEMBL402132 — IC50 = 36.31 nM 7.44
CHEMBL403222 — IC50 = 39.81 nM 7.40
CHEMBL402411 — IC50 = 45.71 nM 7.34
CHEMBL258111 — IC50 = 128.82 nM 6.89
CHEMBL271030 — IC50 = 134.9 nM 6.87
CHEMBL257897 — IC50 = 138.04 nM 6.86
CHEMBL401531 — IC50 = 158.49 nM 6.80
CHEMBL257523 — IC50 = 177.83 nM 6.75
CHEMBL402133 — IC50 = 199.53 nM 6.70
CHEMBL245754 — IC50 = 208.93 nM 6.68
CHEMBL271679 — IC50 = 208.93 nM 6.68
CHEMBL410039 — IC50 = 213.8 nM 6.67
CHEMBL270678 — IC50 = 239.88 nM 6.62
CHEMBL270679 — IC50 = 288.4 nM 6.54
CHEMBL403763 — IC50 = 288.4 nM 6.54
CHEMBL430223 — IC50 = 295.12 nM 6.53
CHEMBL377219 — IC50 = 309.03 nM 6.51
CHEMBL256883 — IC50 = 489.78 nM 6.31
CHEMBL272933 — IC50 = 630.96 nM 6.20
CHEMBL402412 — IC50 = 707.95 nM 6.15
CHEMBL271464 — IC50 = 1023.29 nM 5.99
CHEMBL404091 — IC50 = 1122.02 nM 5.95
CHEMBL270421 — IC50 = 1318.26 nM 5.88
CHEMBL403907 — IC50 = 1380.38 nM 5.86
CHEMBL255638 — IC50 = 2041.74 nM 5.69
CHEMBL270019 — IC50 = 3890.45 nM 5.41
CHEMBL258112 — IC50 = 4897.79 nM 5.31
CHEMBL404339 — IC50 = 5495.41 nM 5.26
CHEMBL271602 — IC50 = 7079.46 nM 5.15
CHEMBL409519 — IC50 = 10471.29 nM 4.98
CHEMBL403105 — IC50 = 10964.78 nM 4.96
CHEMBL257516 — IC50 > 10000.0 nM -
CHEMBL270438 — pIC50 - — -
CHEMBL270436 — pIC50 - — -