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Assay Detail

CHEMBL4737205

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

Binding
Antagonist activity at human P2X3 receptor expressed in rat C6-BU-1 cells
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C6-BU-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 3 (CHEMBL2998) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dioxotriazine derivatives as a new class of P2X receptor antagonists: Identification of a lead and initial SAR studies.
Kai H,Horiguchi T,Kameyama T,Asahi K,Endoh T,Jikihara S,Hasegawa T,Tanaka S,Nozu A,Takeyama C,Tomari M,Takahashi F,Tamura N,Yagi S,Itoh T,Isou Y
Bioorg Med Chem Lett (2021) 37 : 127833 -127833
PubMed 33540044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.12 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494161 — — 1 8.20
CHEMBL3896038 — — 1 8.04
CHEMBL3957828 — — 1 7.96
CHEMBL3984127 — — 1 7.89
CHEMBL3974083 — — 1 7.89
CHEMBL3961985 — — 1 7.85
CHEMBL4748113 — — 1 7.79
CHEMBL3946979 — — 1 7.75
CHEMBL3959782 — — 1 7.70
CHEMBL3969702 — — 1 7.57
CHEMBL3985699 — — 1 7.52
CHEMBL3970466 — — 1 7.51
CHEMBL4789094 — — 1 7.47
CHEMBL3967291 — — 1 7.47
CHEMBL3945216 — — 1 7.42
CHEMBL3946453 — — 1 7.42
CHEMBL3978482 — — 1 7.35
CHEMBL3933324 — — 1 7.34
CHEMBL3968529 — — 1 7.32
CHEMBL3947017 — — 1 7.18
CHEMBL3939178 — — 1 7.11
CHEMBL3921233 — — 1 7.08
CHEMBL3943367 — — 1 7.03
CHEMBL3894513 — — 1 6.89
CHEMBL494833 — — 1 6.87
CHEMBL4746334 — — 1 6.84
CHEMBL4787960 — — 1 6.83
CHEMBL4752152 — — 1 6.82
CHEMBL3922107 — — 1 6.75
CHEMBL4796811 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494161 — IC50 = 6.3 nM 8.20
CHEMBL3896038 — IC50 = 9.1 nM 8.04
CHEMBL3957828 — IC50 = 11.0 nM 7.96
CHEMBL3984127 — IC50 = 13.0 nM 7.89
CHEMBL3974083 — IC50 = 13.0 nM 7.89
CHEMBL3961985 — IC50 = 14.0 nM 7.85
CHEMBL4748113 — IC50 = 16.1 nM 7.79
CHEMBL3946979 — IC50 = 18.0 nM 7.75
CHEMBL3959782 — IC50 = 20.0 nM 7.70
CHEMBL3969702 — IC50 = 27.0 nM 7.57
CHEMBL3985699 — IC50 = 30.3 nM 7.52
CHEMBL3970466 — IC50 = 31.0 nM 7.51
CHEMBL4789094 — IC50 = 34.0 nM 7.47
CHEMBL3967291 — IC50 = 34.0 nM 7.47
CHEMBL3946453 — IC50 = 38.0 nM 7.42
CHEMBL3945216 — IC50 = 38.0 nM 7.42
CHEMBL3978482 — IC50 = 45.0 nM 7.35
CHEMBL3933324 — IC50 = 46.0 nM 7.34
CHEMBL3968529 — IC50 = 48.0 nM 7.32
CHEMBL3947017 — IC50 = 66.0 nM 7.18
CHEMBL3939178 — IC50 = 78.0 nM 7.11
CHEMBL3921233 — IC50 = 83.0 nM 7.08
CHEMBL3943367 — IC50 = 93.0 nM 7.03
CHEMBL3894513 — IC50 = 128.0 nM 6.89
CHEMBL494833 — IC50 = 136.0 nM 6.87
CHEMBL4746334 — IC50 = 144.0 nM 6.84
CHEMBL4787960 — IC50 = 149.0 nM 6.83
CHEMBL4752152 — IC50 = 152.0 nM 6.82
CHEMBL3922107 — IC50 = 176.0 nM 6.75
CHEMBL4796811 — IC50 = 219.0 nM 6.66
CHEMBL3903359 — IC50 = 389.0 nM 6.41
CHEMBL3958610 — IC50 = 415.0 nM 6.38
CHEMBL3912997 — IC50 = 420.0 nM 6.38
CHEMBL3912235 — IC50 = 450.0 nM 6.35
CHEMBL3932555 — IC50 = 520.0 nM 6.28
CHEMBL4788581 — IC50 = 614.0 nM 6.21
CHEMBL3965257 — IC50 = 629.0 nM 6.20
CHEMBL3890959 — IC50 = 953.0 nM 6.02
CHEMBL4749540 — IC50 = 1200.0 nM 5.92
CHEMBL4750833 — IC50 > 3000.0 nM -
CHEMBL4750072 — IC50 > 3000.0 nM -
CHEMBL4797152 — IC50 > 3000.0 nM -
CHEMBL4743578 — IC50 > 3000.0 nM -
CHEMBL4759101 — IC50 > 3000.0 nM -
CHEMBL4783380 — IC50 > 3000.0 nM -
CHEMBL4757743 — IC50 > 3000.0 nM -
CHEMBL4746738 — IC50 > 3000.0 nM -
CHEMBL4753465 — IC50 > 3000.0 nM -
CHEMBL4797969 — IC50 > 1000.0 nM -
CHEMBL4778429 — IC50 > 1000.0 nM -