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Assay Detail

CHEMBL5326672

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

Binding
Activation of rat SK2 variant a transfected in human tsA201 cells coexpressing CaM/GFP in presence of Ca2+ by Fluo-4 staining based electrophysiological method
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type tsA201
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, synthesis and biological evaluation of pyrrolopyrimidine derivatives as novel and selective positive modulator of the small conductance Ca<sup>2+</sup>-activated K<sup>+</sup> channels.
Guo R, Cui M, Li X, Wu M, Xu F, Zhang Y, Wang C, Feng P, Wang J, Huo S, Luo Z, Xing R, Gu J, Shi X, Liu Y, Wang L.
Eur J Med Chem (2023) 254 : 115353 -115353
PubMed 37068385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 5.47 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5403198 1 6.47
CHEMBL5412913 1 6.32
CHEMBL5412532 1 6.30
CHEMBL5402800 1 6.14
CHEMBL5426485 1 5.92
CHEMBL5427458 1 5.80
CHEMBL5438987 1 5.76
CHEMBL5398226 1 5.75
CHEMBL5421015 1 5.74
CHEMBL5408455 1 5.71
CHEMBL5408837 1 5.64
CHEMBL5407203 1 5.53
CHEMBL5423107 1 5.51
CHEMBL5438679 1 5.47
CHEMBL5405151 1 5.46
CHEMBL5440403 1 5.44
CHEMBL5423234 1 5.42
CHEMBL5419617 1 5.39
CHEMBL5414738 1 5.37
CHEMBL5436837 1 5.24
CHEMBL5436262 1 5.19
CHEMBL5407939 1 5.18
CHEMBL5439926 1 5.17
CHEMBL5438952 1 5.11
CHEMBL5407652 1 5.08
CHEMBL5427852 1 5.07
CHEMBL5433086 1 4.86
CHEMBL5412396 1 4.72
CHEMBL5397891 1 4.69
CHEMBL5407100 1 4.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5403198 EC50 = 340.0 nM 6.47
CHEMBL5412913 EC50 = 480.0 nM 6.32
CHEMBL5412532 EC50 = 500.0 nM 6.30
CHEMBL5402800 EC50 = 730.0 nM 6.14
CHEMBL5426485 EC50 = 1200.0 nM 5.92
CHEMBL5427458 EC50 = 1600.0 nM 5.80
CHEMBL5438987 EC50 = 1730.0 nM 5.76
CHEMBL5398226 EC50 = 1790.0 nM 5.75
CHEMBL5421015 EC50 = 1830.0 nM 5.74
CHEMBL5408455 EC50 = 1940.0 nM 5.71
CHEMBL5408837 EC50 = 2280.0 nM 5.64
CHEMBL5407203 EC50 = 2970.0 nM 5.53
CHEMBL5423107 EC50 = 3100.0 nM 5.51
CHEMBL5438679 EC50 = 3410.0 nM 5.47
CHEMBL5405151 EC50 = 3500.0 nM 5.46
CHEMBL5440403 EC50 = 3650.0 nM 5.44
CHEMBL5423234 EC50 = 3810.0 nM 5.42
CHEMBL5419617 EC50 = 4080.0 nM 5.39
CHEMBL5414738 EC50 = 4310.0 nM 5.37
CHEMBL5436837 EC50 = 5730.0 nM 5.24
CHEMBL5436262 EC50 = 6520.0 nM 5.19
CHEMBL5407939 EC50 = 6540.0 nM 5.18
CHEMBL5439926 EC50 = 6780.0 nM 5.17
CHEMBL5438952 EC50 = 7710.0 nM 5.11
CHEMBL5407652 EC50 = 8340.0 nM 5.08
CHEMBL5427852 EC50 = 8430.0 nM 5.07
CHEMBL5433086 EC50 = 13700.0 nM 4.86
CHEMBL5412396 EC50 = 19110.0 nM 4.72
CHEMBL5397891 EC50 = 20400.0 nM 4.69
CHEMBL5407100 EC50 = 29800.0 nM 4.53
CHEMBL5407110 EC50 > 100000.0 nM -
CHEMBL5422240 EC50 > 100000.0 nM -
CHEMBL5402523 EC50 > 100000.0 nM -
CHEMBL5439372 EC50 > 100000.0 nM -
CHEMBL5423423 EC50 > 100000.0 nM -
CHEMBL5416413 EC50 > 100000.0 nM -
CHEMBL5439588 EC50 > 100000.0 nM -
CHEMBL5436322 EC50 > 100000.0 nM -
CHEMBL5409930 EC50 > 100000.0 nM -
CHEMBL5432185 EC50 > 100000.0 nM -