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Assay Detail

CHEMBL4144178

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

Binding
Inhibition of PHD2 in human Hep3B cells assessed as increase in EPO release after 24 hrs by ELISA
22
Total Activities
22
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

Egl nine homolog 1 (CHEMBL5697)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.
Ogoshi Y, Matsui T, Mitani I, Yokota M, Terashita M, Motoda D, Ueyama K, Hotta T, Ito T, Hase Y, Fukui K, Deai K, Yoshiuchi H, Ito S, Abe H.
ACS Med Chem Lett (2017) 8 : 1320 -1325
PubMed 29259755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 4.98 5.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168030 1 5.38
CHEMBL4174643 1 5.35
CHEMBL4164403 1 5.33
CHEMBL4159751 1 5.24
CHEMBL4171201 1 5.24
CHEMBL4175892 1 5.24
CHEMBL4166742 1 5.24
CHEMBL4167844 1 5.03
CHEMBL4175056 1 4.92
CHEMBL4167657 1 4.89
CHEMBL4171371 1 4.85
CHEMBL4173606 1 4.85
CHEMBL4166512 1 4.82
CHEMBL4162891 1 4.77
CHEMBL4163070 1 4.72
CHEMBL4159929 1 4.68
CHEMBL426560 1 4.10
CHEMBL4160770 1 -
CHEMBL4174815 1 -
CHEMBL4164159 1 -
CHEMBL4159695 1 -
CHEMBL4167612 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168030 EC50 = 4200.0 nM 5.38
CHEMBL4174643 EC50 = 4500.0 nM 5.35
CHEMBL4164403 EC50 = 4700.0 nM 5.33
CHEMBL4159751 EC50 = 5800.0 nM 5.24
CHEMBL4171201 EC50 = 5800.0 nM 5.24
CHEMBL4175892 EC50 = 5800.0 nM 5.24
CHEMBL4166742 EC50 = 5700.0 nM 5.24
CHEMBL4167844 EC50 = 9300.0 nM 5.03
CHEMBL4175056 EC50 = 12000.0 nM 4.92
CHEMBL4167657 EC50 = 13000.0 nM 4.89
CHEMBL4171371 EC50 = 14000.0 nM 4.85
CHEMBL4173606 EC50 = 14000.0 nM 4.85
CHEMBL4166512 EC50 = 15000.0 nM 4.82
CHEMBL4162891 EC50 = 17000.0 nM 4.77
CHEMBL4163070 EC50 = 19000.0 nM 4.72
CHEMBL4159929 EC50 = 21000.0 nM 4.68
CHEMBL426560 EC50 = 79000.0 nM 4.10
CHEMBL4160770 EC50 > 30000.0 nM -
CHEMBL4174815 EC50 > 30000.0 nM -
CHEMBL4164159 EC50 > 30000.0 nM -
CHEMBL4159695 EC50 > 30000.0 nM -
CHEMBL4167612 EC50 > 30000.0 nM -