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Assay Detail

CHEMBL5535232

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

Toxicity
Inhibition of hERG expressed in CHO cells at -80 mV holding potential incubated for 7 to 10 mins by automated patch clamp method
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
Baska F, Bozó É, Szeleczky Z, Szántó G, Vukics K, Szakács Z, Domány-Kovács K, Kurkó D, Vass E, Thán M, Vastag M, Temesvári K, Lévai S, Halász AS, Szondiné Kordás K, Román V, Greiner I, Bata I.
J Med Chem (2024) 67 : 643 -673
PubMed 38165765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.02 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5563627 1 5.46
CHEMBL5571665 1 5.46
CHEMBL5579703 1 5.43
CHEMBL5567358 1 5.42
CHEMBL5574495 1 5.40
CHEMBL5571796 1 4.99
CHEMBL5573173 1 4.92
CHEMBL5565555 1 4.89
CHEMBL5575102 1 4.86
CHEMBL5563327 1 4.78
CHEMBL5572381 1 4.72
CHEMBL4297183 BALOVAPTAN 3.0 1 4.68
CHEMBL5573091 1 4.67
CHEMBL5572870 1 4.64
CHEMBL5594885 1 -
CHEMBL5571184 1 -
CHEMBL5542954 1 -
CHEMBL5571560 1 -
CHEMBL5563054 1 -
CHEMBL5573279 1 -
CHEMBL5570369 1 -
CHEMBL5574628 1 -
CHEMBL5574305 1 -
CHEMBL5570415 1 -
CHEMBL5070261 1 -
CHEMBL5070075 1 -
CHEMBL5074709 1 -
CHEMBL5570184 1 -
CHEMBL5574481 1 -
CHEMBL5549819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5563627 IC50 = 3500.0 nM 5.46
CHEMBL5571665 IC50 = 3500.0 nM 5.46
CHEMBL5579703 IC50 = 3700.0 nM 5.43
CHEMBL5567358 IC50 = 3800.0 nM 5.42
CHEMBL5574495 IC50 = 4000.0 nM 5.40
CHEMBL5571796 IC50 = 10200.0 nM 4.99
CHEMBL5573173 IC50 = 12000.0 nM 4.92
CHEMBL5565555 IC50 = 13000.0 nM 4.89
CHEMBL5575102 IC50 = 13800.0 nM 4.86
CHEMBL5563327 IC50 = 16700.0 nM 4.78
CHEMBL5572381 IC50 = 19000.0 nM 4.72
CHEMBL4297183 BALOVAPTAN IC50 = 21000.0 nM 4.68
CHEMBL5573091 IC50 = 21400.0 nM 4.67
CHEMBL5572870 IC50 = 23000.0 nM 4.64
CHEMBL5568795 IC50 - -
CHEMBL5566522 IC50 - -
CHEMBL5569782 IC50 - -
CHEMBL5572998 IC50 - -
CHEMBL5575000 IC50 - -
CHEMBL5565605 IC50 - -
CHEMBL5564603 IC50 - -
CHEMBL5575561 IC50 - -
CHEMBL5573085 IC50 - -
CHEMBL5594885 IC50 > 30000.0 nM -
CHEMBL5571184 IC50 > 30000.0 nM -
CHEMBL5542954 IC50 - -
CHEMBL5571560 IC50 - -
CHEMBL5563054 IC50 - -
CHEMBL5573279 IC50 - -
CHEMBL5570369 IC50 - -
CHEMBL5574628 IC50 - -
CHEMBL5574305 IC50 - -
CHEMBL5570415 IC50 > 30000.0 nM -
CHEMBL5070261 IC50 > 30000.0 nM -
CHEMBL5070075 IC50 > 30000.0 nM -
CHEMBL5074709 IC50 > 30000.0 nM -
CHEMBL5570184 IC50 - -
CHEMBL5574481 IC50 - -
CHEMBL5549819 IC50 - -