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Assay Detail

CHEMBL1028693

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Functional
Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake
ChEMBL ↗
94
Total Activities
94
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Antagonists of the P2X(7) receptor. From lead identification to drug development.
Guile SD, Alcaraz L, Birkinshaw TN, Bowers KC, Ebden MR, Furber M, Stocks MJ.
J Med Chem (2009) 52 : 3123 -3141
PubMed 19191585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 7.58 10.30
Kd 15 7.54 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL550030 — — 1 10.30
CHEMBL560506 — — 1 10.10
CHEMBL551360 — — 1 9.70
CHEMBL564882 — — 1 9.50
CHEMBL551362 — — 1 9.40
CHEMBL556680 — — 1 9.00
CHEMBL550436 — — 1 8.90
CHEMBL441479 — — 1 8.80
CHEMBL340983 — — 1 8.80
CHEMBL560219 — — 1 8.70
CHEMBL552513 — — 1 8.60
CHEMBL552512 — — 1 8.50
CHEMBL564535 — — 1 8.40
CHEMBL341226 — — 1 8.30
CHEMBL131162 — — 1 8.30
CHEMBL563255 — — 1 8.20
CHEMBL563379 — — 1 8.20
CHEMBL551301 — — 1 8.10
CHEMBL336619 — — 1 8.10
CHEMBL424451 — — 1 8.00
CHEMBL551377 — — 1 8.00
CHEMBL497967 — — 1 8.00
CHEMBL562308 — — 1 8.00
CHEMBL257045 — — 1 7.90
CHEMBL210835 — — 1 7.90
CHEMBL437703 — — 1 7.90
CHEMBL563569 — — 1 7.80
CHEMBL560048 — — 1 7.80
CHEMBL555561 — — 1 7.80
CHEMBL380239 — — 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL550030 — IC50 = 0.05012 nM 10.30
CHEMBL560506 — IC50 = 0.07943 nM 10.10
CHEMBL551360 — IC50 = 0.1995 nM 9.70
CHEMBL564882 — IC50 = 0.3162 nM 9.50
CHEMBL551362 — IC50 = 0.3981 nM 9.40
CHEMBL556680 — IC50 = 1.0 nM 9.00
CHEMBL550436 — IC50 = 1.259 nM 8.90
CHEMBL441479 — Kd = 1.585 nM 8.80
CHEMBL340983 — Kd = 1.585 nM 8.80
CHEMBL560219 — IC50 = 1.995 nM 8.70
CHEMBL552513 — IC50 = 2.512 nM 8.60
CHEMBL552512 — IC50 = 3.162 nM 8.50
CHEMBL564535 — IC50 = 3.981 nM 8.40
CHEMBL341226 — Kd = 5.012 nM 8.30
CHEMBL131162 — Kd = 5.012 nM 8.30
CHEMBL563255 — IC50 = 6.31 nM 8.20
CHEMBL563379 — IC50 = 6.31 nM 8.20
CHEMBL551301 — IC50 = 7.943 nM 8.10
CHEMBL336619 — Kd = 7.943 nM 8.10
CHEMBL424451 — Kd = 10.0 nM 8.00
CHEMBL551377 — IC50 = 10.0 nM 8.00
CHEMBL497967 — IC50 = 10.0 nM 8.00
CHEMBL562308 — IC50 = 10.0 nM 8.00
CHEMBL437703 — IC50 = 12.59 nM 7.90
CHEMBL257045 — IC50 = 12.59 nM 7.90
CHEMBL210835 — IC50 = 12.59 nM 7.90
CHEMBL563569 — IC50 = 15.85 nM 7.80
CHEMBL560048 — IC50 = 15.85 nM 7.80
CHEMBL555561 — IC50 = 15.85 nM 7.80
CHEMBL380239 — IC50 = 15.85 nM 7.80
CHEMBL128101 — Kd = 15.85 nM 7.80
CHEMBL271462 — IC50 = 15.85 nM 7.80
CHEMBL564366 — IC50 = 15.85 nM 7.80
CHEMBL270678 — IC50 = 19.95 nM 7.70
CHEMBL549620 — IC50 = 19.95 nM 7.70
CHEMBL338117 — Kd = 19.95 nM 7.70
CHEMBL403222 — IC50 = 19.95 nM 7.70
CHEMBL551707 — IC50 = 25.12 nM 7.60
CHEMBL565027 — IC50 = 25.12 nM 7.60
CHEMBL555033 — IC50 = 25.12 nM 7.60
CHEMBL128634 — Kd = 31.62 nM 7.50
CHEMBL255787 — IC50 = 39.81 nM 7.40
CHEMBL564463 — Kd = 39.81 nM 7.40
CHEMBL551767 — IC50 = 50.12 nM 7.30
CHEMBL560222 — IC50 = 50.12 nM 7.30
CHEMBL551170 — IC50 = 50.12 nM 7.30
CHEMBL564737 — IC50 = 63.1 nM 7.20
CHEMBL557697 — IC50 = 63.1 nM 7.20
CHEMBL245754 — IC50 = 79.43 nM 7.10
CHEMBL560167 — IC50 = 79.43 nM 7.10