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Assay Detail

CHEMBL4827883

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

Binding
Positive allosteric modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as increase in Ach-induced current at -90 mV membrane potential by two electrode voltage-clamp assay
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors.
Wang X, Xiao H, Wang J, Huang Z, Peng G, Xie W, Bian X, Liu H, Shi C, Yang T, Li X, Gao J, Meng Y, Jiang Q, Chen W, Hu F, Wei N, Wang X, Zhang L, Wang K, Sun Q.
J Med Chem (2021) 64 : 12379 -12396
PubMed 34374537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 45 5.46 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257591 — — 1 6.66
CHEMBL429317 AVL-3288 1.0 1 6.16
CHEMBL4879091 — — 1 5.89
CHEMBL4879155 — — 1 5.85
CHEMBL4848354 — — 1 5.77
CHEMBL4850620 — — 1 5.72
CHEMBL4851790 — — 1 5.70
CHEMBL4859088 — — 1 5.58
CHEMBL4855398 — — 1 5.58
CHEMBL4854969 — — 1 5.52
CHEMBL412119 — — 1 5.50
CHEMBL4876535 — — 1 5.50
CHEMBL4870919 — — 1 5.48
CHEMBL407217 — — 1 5.47
CHEMBL4859301 — — 1 5.47
CHEMBL4875280 — — 1 5.42
CHEMBL4859649 — — 1 5.37
CHEMBL4862000 — — 1 5.37
CHEMBL4848061 — — 1 5.36
CHEMBL4858715 — — 1 5.35
CHEMBL4856836 — — 1 5.27
CHEMBL4872252 — — 1 5.25
CHEMBL4857179 — — 1 5.19
CHEMBL4864500 — — 1 5.17
CHEMBL4846600 — — 1 5.11
CHEMBL4849527 — — 1 5.10
CHEMBL4864054 — — 1 5.08
CHEMBL4870388 — — 1 4.93
CHEMBL1462302 — — 1 4.47
CHEMBL4850272 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257591 — EC50 = 220.0 nM 6.66
CHEMBL429317 AVL-3288 EC50 = 700.0 nM 6.16
CHEMBL4879091 — EC50 = 1300.0 nM 5.89
CHEMBL4879155 — EC50 = 1400.0 nM 5.85
CHEMBL4848354 — EC50 = 1700.0 nM 5.77
CHEMBL4850620 — EC50 = 1900.0 nM 5.72
CHEMBL4851790 — EC50 = 2000.0 nM 5.70
CHEMBL4859088 — EC50 = 2600.0 nM 5.58
CHEMBL4855398 — EC50 = 2600.0 nM 5.58
CHEMBL4854969 — EC50 = 3000.0 nM 5.52
CHEMBL412119 — EC50 = 3162.28 nM 5.50
CHEMBL4876535 — EC50 = 3200.0 nM 5.50
CHEMBL4870919 — EC50 = 3300.0 nM 5.48
CHEMBL407217 — EC50 = 3400.0 nM 5.47
CHEMBL4859301 — EC50 = 3400.0 nM 5.47
CHEMBL4875280 — EC50 = 3800.0 nM 5.42
CHEMBL4859649 — EC50 = 4300.0 nM 5.37
CHEMBL4862000 — EC50 = 4300.0 nM 5.37
CHEMBL4848061 — EC50 = 4400.0 nM 5.36
CHEMBL4858715 — EC50 = 4500.0 nM 5.35
CHEMBL4856836 — EC50 = 5400.0 nM 5.27
CHEMBL4872252 — EC50 = 5600.0 nM 5.25
CHEMBL4857179 — EC50 = 6400.0 nM 5.19
CHEMBL4864500 — EC50 = 6700.0 nM 5.17
CHEMBL4846600 — EC50 = 7700.0 nM 5.11
CHEMBL4849527 — EC50 = 7900.0 nM 5.10
CHEMBL4864054 — EC50 = 8300.0 nM 5.08
CHEMBL4870388 — EC50 = 11700.0 nM 4.93
CHEMBL1462302 — EC50 = 34000.0 nM 4.47
CHEMBL4872273 — EC50 - — -
CHEMBL4873016 — EC50 - — -
CHEMBL4852719 — EC50 - — -
CHEMBL4849228 — EC50 - — -
CHEMBL4858979 — EC50 - — -
CHEMBL4863956 — EC50 - — -
CHEMBL4858202 — EC50 - — -
CHEMBL4866699 — EC50 - — -
CHEMBL4852634 — EC50 - — -
CHEMBL4877787 — EC50 - — -
CHEMBL4861958 — EC50 - — -
CHEMBL4856930 — EC50 - — -
CHEMBL4874026 — EC50 - — -
CHEMBL4861330 — EC50 - — -
CHEMBL4868308 — EC50 - — -
CHEMBL4850272 — EC50 - — -