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Assay Detail

CHEMBL1780986

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Functional
Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
Perez-Medrano A, Donnelly-Roberts DL, Florjancic AS, Nelson DW, Li T, Namovic MT, Peddi S, Faltynek CR, Jarvis MF, Carroll WA.
Bioorg Med Chem Lett (2011) 21 : 3297 -3300
PubMed 21536435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.33 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1778008 — — 1 7.94
CHEMBL1778009 — — 1 7.86
CHEMBL1778011 — — 1 7.84
CHEMBL1778114 — — 1 7.83
CHEMBL1778113 — — 1 7.83
CHEMBL1778121 — — 1 7.80
CHEMBL1778012 — — 1 7.78
CHEMBL1778013 — — 1 7.78
CHEMBL380239 — — 1 7.75
CHEMBL1778014 — — 1 7.74
CHEMBL1778017 — — 1 7.74
CHEMBL1778123 — — 1 7.70
CHEMBL1778115 — — 1 7.70
CHEMBL402133 — — 1 7.68
CHEMBL1778126 — — 1 7.68
CHEMBL1778015 — — 1 7.66
CHEMBL1778019 — — 1 7.62
CHEMBL1778018 — — 1 7.62
CHEMBL1778124 — — 1 7.57
CHEMBL1778020 — — 1 7.56
CHEMBL1778021 — — 1 7.55
CHEMBL1778116 — — 1 7.55
CHEMBL1778122 — — 1 7.53
CHEMBL1778118 — — 1 7.52
CHEMBL1778022 — — 1 7.50
CHEMBL1778025 — — 1 7.50
CHEMBL1778125 — — 1 7.41
CHEMBL1778016 — — 1 7.40
CHEMBL1778010 — — 1 7.39
CHEMBL1778117 — — 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1778008 — IC50 = 11.48 nM 7.94
CHEMBL1778009 — IC50 = 13.8 nM 7.86
CHEMBL1778011 — IC50 = 14.45 nM 7.84
CHEMBL1778114 — IC50 = 14.79 nM 7.83
CHEMBL1778113 — IC50 = 14.79 nM 7.83
CHEMBL1778121 — IC50 = 15.85 nM 7.80
CHEMBL1778012 — IC50 = 16.6 nM 7.78
CHEMBL1778013 — IC50 = 16.6 nM 7.78
CHEMBL380239 — IC50 = 17.78 nM 7.75
CHEMBL1778014 — IC50 = 18.2 nM 7.74
CHEMBL1778017 — IC50 = 18.2 nM 7.74
CHEMBL1778115 — IC50 = 19.95 nM 7.70
CHEMBL1778123 — IC50 = 19.95 nM 7.70
CHEMBL402133 — IC50 = 20.89 nM 7.68
CHEMBL1778126 — IC50 = 20.89 nM 7.68
CHEMBL1778015 — IC50 = 21.88 nM 7.66
CHEMBL1778019 — IC50 = 23.99 nM 7.62
CHEMBL1778018 — IC50 = 23.99 nM 7.62
CHEMBL1778124 — IC50 = 26.92 nM 7.57
CHEMBL1778020 — IC50 = 27.54 nM 7.56
CHEMBL1778021 — IC50 = 28.18 nM 7.55
CHEMBL1778116 — IC50 = 28.18 nM 7.55
CHEMBL1778122 — IC50 = 29.51 nM 7.53
CHEMBL1778118 — IC50 = 30.2 nM 7.52
CHEMBL1778022 — IC50 = 31.62 nM 7.50
CHEMBL1778025 — IC50 = 31.62 nM 7.50
CHEMBL1778125 — IC50 = 38.9 nM 7.41
CHEMBL1778016 — IC50 = 39.81 nM 7.40
CHEMBL1778010 — IC50 = 40.74 nM 7.39
CHEMBL1778117 — IC50 = 54.95 nM 7.26
CHEMBL1778023 — IC50 = 54.95 nM 7.26
CHEMBL1778119 — IC50 = 70.79 nM 7.15
CHEMBL1778110 — IC50 = 74.13 nM 7.13
CHEMBL1778107 — IC50 = 74.13 nM 7.13
CHEMBL245754 — IC50 = 77.62 nM 7.11
CHEMBL1778120 — IC50 = 87.1 nM 7.06
CHEMBL1778024 — IC50 = 109.65 nM 6.96
CHEMBL1778026 — IC50 = 120.23 nM 6.92
CHEMBL377219 — IC50 = 123.03 nM 6.91
CHEMBL1778108 — IC50 = 234.42 nM 6.63
CHEMBL1778027 — IC50 = 257.04 nM 6.59
CHEMBL1778109 — IC50 = 436.52 nM 6.36
CHEMBL1778111 — IC50 = 562.34 nM 6.25
CHEMBL1778112 — IC50 = 1905.46 nM 5.72
CHEMBL1778127 — IC50 = 5623.41 nM 5.25