Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1780987

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

Functional
Antagonist activity at rat 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 Rattus norvegicus
Cell Type HEK293
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 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 6.72 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1778113 — — 1 7.73
CHEMBL1778008 — — 1 7.67
CHEMBL1778013 — — 1 7.37
CHEMBL1778018 — — 1 7.36
CHEMBL1778021 — — 1 7.34
CHEMBL1778012 — — 1 7.30
CHEMBL1778011 — — 1 7.26
CHEMBL1778009 — — 1 7.25
CHEMBL1778015 — — 1 7.25
CHEMBL1778121 — — 1 7.23
CHEMBL1778020 — — 1 7.16
CHEMBL380239 — — 1 7.16
CHEMBL1778022 — — 1 7.14
CHEMBL1778014 — — 1 7.12
CHEMBL1778019 — — 1 6.99
CHEMBL1778017 — — 1 6.99
CHEMBL1778025 — — 1 6.98
CHEMBL1778023 — — 1 6.97
CHEMBL1778024 — — 1 6.94
CHEMBL1778107 — — 1 6.92
CHEMBL1778016 — — 1 6.90
CHEMBL1778118 — — 1 6.85
CHEMBL1778124 — — 1 6.84
CHEMBL1778114 — — 1 6.82
CHEMBL1778010 — — 1 6.76
CHEMBL1778110 — — 1 6.73
CHEMBL1778123 — — 1 6.70
CHEMBL402133 — — 1 6.70
CHEMBL245754 — — 1 6.68
CHEMBL1778115 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1778113 — IC50 = 18.62 nM 7.73
CHEMBL1778008 — IC50 = 21.38 nM 7.67
CHEMBL1778013 — IC50 = 42.66 nM 7.37
CHEMBL1778018 — IC50 = 43.65 nM 7.36
CHEMBL1778021 — IC50 = 45.71 nM 7.34
CHEMBL1778012 — IC50 = 50.12 nM 7.30
CHEMBL1778011 — IC50 = 54.95 nM 7.26
CHEMBL1778009 — IC50 = 56.23 nM 7.25
CHEMBL1778015 — IC50 = 56.23 nM 7.25
CHEMBL1778121 — IC50 = 58.88 nM 7.23
CHEMBL1778020 — IC50 = 69.18 nM 7.16
CHEMBL380239 — IC50 = 69.18 nM 7.16
CHEMBL1778022 — IC50 = 72.44 nM 7.14
CHEMBL1778014 — IC50 = 75.86 nM 7.12
CHEMBL1778017 — IC50 = 102.33 nM 6.99
CHEMBL1778019 — IC50 = 102.33 nM 6.99
CHEMBL1778025 — IC50 = 104.71 nM 6.98
CHEMBL1778023 — IC50 = 107.15 nM 6.97
CHEMBL1778024 — IC50 = 114.82 nM 6.94
CHEMBL1778107 — IC50 = 120.23 nM 6.92
CHEMBL1778016 — IC50 = 125.89 nM 6.90
CHEMBL1778118 — IC50 = 141.25 nM 6.85
CHEMBL1778124 — IC50 = 144.54 nM 6.84
CHEMBL1778114 — IC50 = 151.36 nM 6.82
CHEMBL1778010 — IC50 = 173.78 nM 6.76
CHEMBL1778110 — IC50 = 186.21 nM 6.73
CHEMBL1778123 — IC50 = 199.53 nM 6.70
CHEMBL402133 — IC50 = 199.53 nM 6.70
CHEMBL245754 — IC50 = 208.93 nM 6.68
CHEMBL1778115 — IC50 = 218.78 nM 6.66
CHEMBL1778117 — IC50 = 229.09 nM 6.64
CHEMBL1778116 — IC50 = 245.47 nM 6.61
CHEMBL1778122 — IC50 = 288.4 nM 6.54
CHEMBL377219 — IC50 = 309.03 nM 6.51
CHEMBL1778026 — IC50 = 467.74 nM 6.33
CHEMBL1778119 — IC50 = 524.81 nM 6.28
CHEMBL1778120 — IC50 = 794.33 nM 6.10
CHEMBL1778125 — IC50 = 794.33 nM 6.10
CHEMBL1778126 — IC50 = 831.76 nM 6.08
CHEMBL1778027 — IC50 = 933.25 nM 6.03
CHEMBL1778111 — IC50 = 954.99 nM 6.02
CHEMBL1778108 — IC50 = 1023.29 nM 5.99
CHEMBL1778127 — IC50 = 3630.78 nM 5.44
CHEMBL1778109 — IC50 = 7079.46 nM 5.15
CHEMBL1778112 — IC50 = 15848.93 nM 4.80