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Assay Detail

CHEMBL854892

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Binding
Inhibition of binding to hERG
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Meyers KM, Kim N, Méndez-Andino JL, Hu XE, Mumin RN, Klopfenstein SR, Wos JA, Mitchell MC, Paris JL, Ackley DC, Holbert JK, Mittelstadt SW, Reizes O.
Bioorg Med Chem Lett (2007) 17 : 814 -818
PubMed 17107791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.20 5.75
IC25 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214432 1 5.75
CHEMBL216821 1 5.75
CHEMBL215278 1 5.58
CHEMBL424895 1 5.30
CHEMBL217820 1 5.29
CHEMBL215660 1 5.28
CHEMBL437728 1 5.17
CHEMBL216314 1 5.00
CHEMBL216741 1 4.85
CHEMBL216406 1 4.70
CHEMBL267320 1 4.52
CHEMBL217860 1 -
CHEMBL214178 1 -
CHEMBL213771 1 -
CHEMBL268848 1 -
CHEMBL217501 1 -
CHEMBL216429 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214432 IC50 = 1800.0 nM 5.75
CHEMBL216821 IC50 = 1800.0 nM 5.75
CHEMBL215278 IC50 = 2600.0 nM 5.58
CHEMBL424895 IC50 = 5000.0 nM 5.30
CHEMBL217820 IC50 = 5100.0 nM 5.29
CHEMBL215660 IC50 = 5200.0 nM 5.28
CHEMBL437728 IC50 = 6700.0 nM 5.17
CHEMBL216314 IC50 = 10000.0 nM 5.00
CHEMBL216741 IC50 = 14000.0 nM 4.85
CHEMBL216406 IC50 = 20000.0 nM 4.70
CHEMBL267320 IC50 = 30000.0 nM 4.52
CHEMBL217860 IC25 = 2.5 uM -
CHEMBL214178 IC25 = 7.6 uM -
CHEMBL213771 IC25 = 14.0 uM -
CHEMBL268848 IC25 = 20.0 uM -
CHEMBL217501 IC25 = 30.0 uM -
CHEMBL216429 IC25 = 34.0 uM -