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Assay Detail

CHEMBL886454

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Functional
Antagonist activity at human recombinant P2X7 receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2X purinoceptor 7 (CHEMBL4805)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Carroll WA, Kalvin DM, Perez Medrano A, Florjancic AS, Wang Y, Donnelly-Roberts DL, Namovic MT, Grayson G, Honoré P, Jarvis MF.
Bioorg Med Chem Lett (2007) 17 : 4044 -4048
PubMed 17482819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.62 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393241 1 7.72
CHEMBL396587 1 7.57
CHEMBL208560 1 7.40
CHEMBL247586 1 7.32
CHEMBL245561 1 7.31
CHEMBL247782 1 7.31
CHEMBL246578 1 7.30
CHEMBL245758 1 7.23
CHEMBL441479 1 7.19
CHEMBL245754 1 7.11
CHEMBL245560 1 6.93
CHEMBL245972 1 6.88
CHEMBL245756 1 6.88
CHEMBL246172 1 6.86
CHEMBL245562 1 6.84
CHEMBL245973 1 6.72
CHEMBL245755 1 6.72
CHEMBL246770 1 6.68
CHEMBL245578 1 6.67
CHEMBL392216 1 6.52
CHEMBL392171 1 6.48
CHEMBL393485 1 6.37
CHEMBL265896 1 6.28
CHEMBL246767 1 6.22
CHEMBL391960 1 6.04
CHEMBL246173 1 5.98
CHEMBL392170 1 5.89
CHEMBL429110 1 5.74
CHEMBL393684 1 5.22
CHEMBL245775 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393241 IC50 = 19.05 nM 7.72
CHEMBL396587 IC50 = 26.92 nM 7.57
CHEMBL208560 IC50 = 39.81 nM 7.40
CHEMBL247586 IC50 = 47.86 nM 7.32
CHEMBL245561 IC50 = 48.98 nM 7.31
CHEMBL247782 IC50 = 48.98 nM 7.31
CHEMBL246578 IC50 = 50.12 nM 7.30
CHEMBL245758 IC50 = 58.88 nM 7.23
CHEMBL441479 IC50 = 64.57 nM 7.19
CHEMBL245754 IC50 = 77.62 nM 7.11
CHEMBL245560 IC50 = 117.49 nM 6.93
CHEMBL245972 IC50 = 131.83 nM 6.88
CHEMBL245756 IC50 = 131.83 nM 6.88
CHEMBL246172 IC50 = 138.04 nM 6.86
CHEMBL245562 IC50 = 144.54 nM 6.84
CHEMBL245973 IC50 = 190.55 nM 6.72
CHEMBL245755 IC50 = 190.55 nM 6.72
CHEMBL246770 IC50 = 208.93 nM 6.68
CHEMBL245578 IC50 = 213.8 nM 6.67
CHEMBL392216 IC50 = 302.0 nM 6.52
CHEMBL392171 IC50 = 331.13 nM 6.48
CHEMBL393485 IC50 = 426.58 nM 6.37
CHEMBL265896 IC50 = 524.81 nM 6.28
CHEMBL246767 IC50 = 602.56 nM 6.22
CHEMBL391960 IC50 = 912.01 nM 6.04
CHEMBL246173 IC50 = 1047.13 nM 5.98
CHEMBL392170 IC50 = 1288.25 nM 5.89
CHEMBL429110 IC50 = 1819.7 nM 5.74
CHEMBL393684 IC50 = 6025.6 nM 5.22
CHEMBL245775 IC50 = 8912.51 nM 5.05
CHEMBL246375 IC50 = 13182.57 nM 4.88