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Assay Detail

CHEMBL916228

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

Functional
Inhibition of hypoxia induced HIF1 transcriptional activity in human Hep3B cells by cell-based HRE reporter assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Hep 3B2
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha (CHEMBL2221345)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

(Aryloxyacetylamino)benzoic acid analogues: A new class of hypoxia-inducible factor-1 inhibitors.
Lee K, Lee JH, Boovanahalli SK, Jin Y, Lee M, Jin X, Kim JH, Hong YS, Lee JJ.
J Med Chem (2007) 50 : 1675 -1684
PubMed 17328532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.13 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223862 1 6.40
CHEMBL427092 1 5.58
CHEMBL222606 1 5.37
CHEMBL219673 1 5.30
CHEMBL221659 1 5.14
CHEMBL224964 1 5.09
CHEMBL373396 1 5.00
CHEMBL222873 1 4.98
CHEMBL374484 1 4.90
CHEMBL333985 1 4.86
CHEMBL373657 1 4.85
CHEMBL222637 1 4.63
CHEMBL223235 1 4.54
CHEMBL415056 1 -
CHEMBL222089 1 -
CHEMBL374776 1 -
CHEMBL223154 1 -
CHEMBL373912 1 -
CHEMBL221560 1 -
CHEMBL222422 1 -
CHEMBL376203 1 -
CHEMBL222657 1 -
CHEMBL222607 1 -
CHEMBL375173 1 -
CHEMBL223305 1 -
CHEMBL222754 1 -
CHEMBL222582 1 -
CHEMBL374969 1 -
CHEMBL223479 1 -
CHEMBL222251 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223862 IC50 = 400.0 nM 6.40
CHEMBL427092 IC50 = 2600.0 nM 5.58
CHEMBL222606 IC50 = 4300.0 nM 5.37
CHEMBL219673 IC50 = 5000.0 nM 5.30
CHEMBL221659 IC50 = 7200.0 nM 5.14
CHEMBL224964 IC50 = 8200.0 nM 5.09
CHEMBL373396 IC50 = 9900.0 nM 5.00
CHEMBL222873 IC50 = 10500.0 nM 4.98
CHEMBL374484 IC50 = 12600.0 nM 4.90
CHEMBL333985 IC50 = 13800.0 nM 4.86
CHEMBL373657 IC50 = 14080.0 nM 4.85
CHEMBL222637 IC50 = 23200.0 nM 4.63
CHEMBL223235 IC50 = 29000.0 nM 4.54
CHEMBL222104 IC50 > 30000.0 nM -
CHEMBL222879 IC50 > 30000.0 nM -
CHEMBL224750 IC50 > 30000.0 nM -
CHEMBL415056 IC50 > 30000.0 nM -
CHEMBL222089 IC50 > 30000.0 nM -
CHEMBL374776 IC50 > 30000.0 nM -
CHEMBL223154 IC50 > 30000.0 nM -
CHEMBL373912 IC50 > 30000.0 nM -
CHEMBL221560 IC50 > 30000.0 nM -
CHEMBL222422 IC50 > 30000.0 nM -
CHEMBL376203 IC50 > 30000.0 nM -
CHEMBL222657 IC50 > 30000.0 nM -
CHEMBL222607 IC50 > 30000.0 nM -
CHEMBL375173 IC50 > 30000.0 nM -
CHEMBL223305 IC50 > 30000.0 nM -
CHEMBL222754 IC50 > 30000.0 nM -
CHEMBL222582 IC50 > 30000.0 nM -
CHEMBL374969 IC50 > 30000.0 nM -
CHEMBL223479 IC50 > 30000.0 nM -
CHEMBL222251 IC50 > 30000.0 nM -