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Assay Detail

CHEMBL5041445

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

Binding
Potentiation of rat KCa2.2a expressed in HEK293 cells at -90 mV holding potential measured at 1 to 2 days by patch clamp electrophysiology
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structure-Activity Relationship Study of Subtype-Selective Positive Modulators of K<sub>Ca</sub>2 Channels.
El-Sayed NS, Nam YW, Egorova PA, Nguyen HM, Orfali R, Rahman MA, Yang G, Wulff H, Bezprozvanny I, Parang K, Zhang M.
J Med Chem (2022) 65 : 303 -322
PubMed 34962403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 5.34 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5086997 1 6.19
CHEMBL5078247 1 6.00
CHEMBL5074700 1 5.72
CHEMBL5076878 1 5.70
CHEMBL5076032 1 5.53
CHEMBL5081906 1 5.49
CHEMBL5075016 1 5.46
CHEMBL5077913 1 5.45
CHEMBL5094656 1 5.37
CHEMBL5079766 1 5.35
CHEMBL5082158 1 5.30
CHEMBL5088936 1 5.18
CHEMBL453730 1 5.13
CHEMBL5094693 1 4.86
CHEMBL5088498 1 4.41
CHEMBL5074647 1 4.30
CHEMBL5072517 1 -
CHEMBL5088379 1 -
CHEMBL5079837 1 -
CHEMBL5086120 1 -
CHEMBL5090801 1 -
CHEMBL5076140 1 -
CHEMBL5090420 1 -
CHEMBL5079951 1 -
CHEMBL5075803 1 -
CHEMBL5084004 1 -
CHEMBL5075501 1 -
CHEMBL5084258 1 -
CHEMBL5090455 1 -
CHEMBL5093708 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5086997 EC50 = 640.0 nM 6.19
CHEMBL5078247 EC50 = 990.0 nM 6.00
CHEMBL5074700 EC50 = 1890.0 nM 5.72
CHEMBL5076878 EC50 = 1990.0 nM 5.70
CHEMBL5076032 EC50 = 2970.0 nM 5.53
CHEMBL5081906 EC50 = 3270.0 nM 5.49
CHEMBL5075016 EC50 = 3450.0 nM 5.46
CHEMBL5077913 EC50 = 3590.0 nM 5.45
CHEMBL5094656 EC50 = 4320.0 nM 5.37
CHEMBL5079766 EC50 = 4510.0 nM 5.35
CHEMBL5082158 EC50 = 5030.0 nM 5.30
CHEMBL5088936 EC50 = 6590.0 nM 5.18
CHEMBL453730 EC50 = 7480.0 nM 5.13
CHEMBL5094693 EC50 = 13770.0 nM 4.86
CHEMBL5088498 EC50 = 38810.0 nM 4.41
CHEMBL5074647 EC50 = 49720.0 nM 4.30
CHEMBL5069418 EC50 > 100000.0 nM -
CHEMBL5079218 EC50 > 100000.0 nM -
CHEMBL5088689 EC50 > 100000.0 nM -
CHEMBL5089976 EC50 > 100000.0 nM -
CHEMBL5081876 EC50 > 100000.0 nM -
CHEMBL5083279 EC50 > 100000.0 nM -
CHEMBL5080805 EC50 > 100000.0 nM -
CHEMBL5093708 EC50 > 100000.0 nM -
CHEMBL5090455 EC50 > 100000.0 nM -
CHEMBL5084258 EC50 > 100000.0 nM -
CHEMBL5075501 EC50 > 100000.0 nM -
CHEMBL5084004 EC50 > 100000.0 nM -
CHEMBL5075803 EC50 > 100000.0 nM -
CHEMBL5079951 EC50 > 100000.0 nM -
CHEMBL5090420 EC50 > 100000.0 nM -
CHEMBL5076140 EC50 > 100000.0 nM -
CHEMBL5090801 EC50 > 30000.0 nM -
CHEMBL5086120 EC50 > 100000.0 nM -
CHEMBL5079837 EC50 > 100000.0 nM -
CHEMBL5088379 EC50 > 100000.0 nM -
CHEMBL5072517 EC50 > 100000.0 nM -