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Assay Detail

CHEMBL970589

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Functional
Antagonist activity at rat cloned P2X7 receptor expressed in HEK293 cells assessed as inhibition of calcium flux by FLIPR assay
ChEMBL ↗
61
Total Activities
59
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

Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.
Perez-Medrano A, Donnelly-Roberts DL, Honore P, Hsieh GC, Namovic MT, Peddi S, Shuai Q, Wang Y, Faltynek CR, Jarvis MF, Carroll WA.
J Med Chem (2009) 52 : 3366 -3376
PubMed 19397270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 61 7.32 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490117 — — 1 8.50
CHEMBL491916 — — 1 8.20
CHEMBL491933 — — 1 8.20
CHEMBL490741 — — 1 8.10
CHEMBL490118 — — 1 8.10
CHEMBL489916 — — 1 8.10
CHEMBL515918 — — 1 8.10
CHEMBL524108 — — 1 8.00
CHEMBL490912 — — 1 8.00
CHEMBL491781 — — 1 8.00
CHEMBL523112 — — 1 7.90
CHEMBL255536 — — 3 7.90
CHEMBL490917 — — 1 7.90
CHEMBL522647 — — 1 7.70
CHEMBL489917 — — 1 7.70
CHEMBL522955 — — 1 7.70
CHEMBL492101 — — 1 7.70
CHEMBL255787 — — 1 7.70
CHEMBL491369 — — 1 7.70
CHEMBL493437 — — 1 7.70
CHEMBL491741 — — 1 7.60
CHEMBL491552 — — 1 7.60
CHEMBL521962 — — 1 7.50
CHEMBL491102 — — 1 7.50
CHEMBL490558 — — 1 7.50
CHEMBL491103 — — 1 7.50
CHEMBL489741 — — 1 7.50
CHEMBL522120 — — 1 7.50
CHEMBL489714 — — 1 7.50
CHEMBL490918 — — 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490117 — IC50 = 3.162 nM 8.50
CHEMBL491916 — IC50 = 6.31 nM 8.20
CHEMBL491933 — IC50 = 6.31 nM 8.20
CHEMBL490741 — IC50 = 7.943 nM 8.10
CHEMBL515918 — IC50 = 7.943 nM 8.10
CHEMBL490118 — IC50 = 7.943 nM 8.10
CHEMBL489916 — IC50 = 7.943 nM 8.10
CHEMBL524108 — IC50 = 10.0 nM 8.00
CHEMBL491781 — IC50 = 10.0 nM 8.00
CHEMBL490912 — IC50 = 10.0 nM 8.00
CHEMBL523112 — IC50 = 12.59 nM 7.90
CHEMBL255536 — IC50 = 12.59 nM 7.90
CHEMBL490917 — IC50 = 12.59 nM 7.90
CHEMBL255536 — IC50 = 12.59 nM 7.90
CHEMBL489917 — IC50 = 19.95 nM 7.70
CHEMBL522955 — IC50 = 19.95 nM 7.70
CHEMBL492101 — IC50 = 19.95 nM 7.70
CHEMBL255787 — IC50 = 19.95 nM 7.70
CHEMBL493437 — IC50 = 19.95 nM 7.70
CHEMBL491369 — IC50 = 19.95 nM 7.70
CHEMBL522647 — IC50 = 19.95 nM 7.70
CHEMBL491741 — IC50 = 25.12 nM 7.60
CHEMBL491552 — IC50 = 25.12 nM 7.60
CHEMBL491102 — IC50 = 31.62 nM 7.50
CHEMBL521962 — IC50 = 31.62 nM 7.50
CHEMBL490558 — IC50 = 31.62 nM 7.50
CHEMBL489741 — IC50 = 31.62 nM 7.50
CHEMBL489714 — IC50 = 31.62 nM 7.50
CHEMBL490918 — IC50 = 31.62 nM 7.50
CHEMBL491103 — IC50 = 31.62 nM 7.50
CHEMBL522120 — IC50 = 31.62 nM 7.50
CHEMBL493436 — IC50 = 39.81 nM 7.40
CHEMBL523319 — IC50 = 39.81 nM 7.40
CHEMBL491553 — IC50 = 39.81 nM 7.40
CHEMBL491740 — IC50 = 39.81 nM 7.40
CHEMBL491934 — IC50 = 39.81 nM 7.40
CHEMBL473020 — IC50 = 39.81 nM 7.40
CHEMBL240177 — IC50 = 50.12 nM 7.30
CHEMBL504419 — IC50 = 50.12 nM 7.30
CHEMBL491907 — IC50 = 50.12 nM 7.30
CHEMBL492113 — IC50 = 50.12 nM 7.30
CHEMBL522967 — IC50 = 63.1 nM 7.20
CHEMBL475368 — IC50 = 79.43 nM 7.10
CHEMBL491730 — IC50 = 100.0 nM 7.00
CHEMBL523478 — IC50 = 100.0 nM 7.00
CHEMBL540965 — IC50 = 125.89 nM 6.90
CHEMBL474645 — IC50 = 158.49 nM 6.80
CHEMBL490696 — IC50 = 158.49 nM 6.80
CHEMBL491713 — IC50 = 199.53 nM 6.70
CHEMBL491728 — IC50 = 199.53 nM 6.70