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Assay Detail

CHEMBL4057174

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

Functional
Inhibition of human recombinant BMP6-stimulated hepcidin mRNA expression in human HepG2 cells after 6 hrs by qRT-PCR analysis
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

HepG2 (CHEMBL395)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of DS79182026: A potent orally active hepcidin production inhibitor.
Fukuda T, Goto R, Kiho T, Ueda K, Muramatsu S, Hashimoto M, Aki A, Watanabe K, Tanaka N.
Bioorg Med Chem Lett (2017) 27 : 3716 -3722
PubMed 28705644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.30 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066592 1 7.41
CHEMBL4088809 1 7.40
CHEMBL4062692 1 7.38
CHEMBL4061521 1 7.33
CHEMBL4080212 1 7.16
CHEMBL4077543 1 7.09
CHEMBL4063674 1 6.89
CHEMBL4067574 1 6.80
CHEMBL4081873 1 6.68
CHEMBL4064948 1 6.68
CHEMBL4095072 1 6.64
CHEMBL4076209 1 6.58
CHEMBL4088455 1 6.54
CHEMBL4084323 1 6.48
CHEMBL4099876 1 6.46
CHEMBL4074063 1 6.40
CHEMBL260163 1 6.40
CHEMBL4080955 1 6.34
CHEMBL4094132 1 6.27
CHEMBL4105203 1 6.24
CHEMBL4092643 1 6.14
CHEMBL4097501 1 6.04
CHEMBL4103763 1 6.00
CHEMBL4078504 1 5.96
CHEMBL4096531 1 5.92
CHEMBL4061027 1 5.85
CHEMBL4084374 1 5.58
CHEMBL4100824 1 5.58
CHEMBL4067606 1 5.54
CHEMBL4092127 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066592 IC50 = 39.0 nM 7.41
CHEMBL4088809 IC50 = 40.0 nM 7.40
CHEMBL4062692 IC50 = 42.0 nM 7.38
CHEMBL4061521 IC50 = 47.0 nM 7.33
CHEMBL4080212 IC50 = 69.0 nM 7.16
CHEMBL4077543 IC50 = 82.0 nM 7.09
CHEMBL4063674 IC50 = 130.0 nM 6.89
CHEMBL4067574 IC50 = 160.0 nM 6.80
CHEMBL4081873 IC50 = 210.0 nM 6.68
CHEMBL4064948 IC50 = 210.0 nM 6.68
CHEMBL4095072 IC50 = 230.0 nM 6.64
CHEMBL4076209 IC50 = 260.0 nM 6.58
CHEMBL4088455 IC50 = 290.0 nM 6.54
CHEMBL4084323 IC50 = 330.0 nM 6.48
CHEMBL4099876 IC50 = 350.0 nM 6.46
CHEMBL4074063 IC50 = 400.0 nM 6.40
CHEMBL260163 IC50 = 400.0 nM 6.40
CHEMBL4080955 IC50 = 460.0 nM 6.34
CHEMBL4094132 IC50 = 540.0 nM 6.27
CHEMBL4105203 IC50 = 580.0 nM 6.24
CHEMBL4092643 IC50 = 720.0 nM 6.14
CHEMBL4097501 IC50 = 910.0 nM 6.04
CHEMBL4103763 IC50 = 1000.0 nM 6.00
CHEMBL4078504 IC50 = 1100.0 nM 5.96
CHEMBL4096531 IC50 = 1200.0 nM 5.92
CHEMBL4061027 IC50 = 1400.0 nM 5.85
CHEMBL4084374 IC50 = 2600.0 nM 5.58
CHEMBL4100824 IC50 = 2600.0 nM 5.58
CHEMBL4092127 IC50 = 2900.0 nM 5.54
CHEMBL4067606 IC50 = 2900.0 nM 5.54
CHEMBL4088833 IC50 = 4400.0 nM 5.36
CHEMBL4071333 IC50 = 4800.0 nM 5.32
CHEMBL4072578 IC50 = 7200.0 nM 5.14
CHEMBL4104204 IC50 = 11000.0 nM 4.96
CHEMBL4070324 IC50 > 10000.0 nM -
CHEMBL4080886 IC50 > 30000.0 nM -
CHEMBL4105124 IC50 > 30000.0 nM -
CHEMBL4070424 IC50 > 3000.0 nM -