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Assay Detail

CHEMBL4010988

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

Binding
Inhibition of HIF-1 pathway in human LN229 cells harboring HRE-AP assessed sa reduction in VEGF transcription pretreated for 1 hr under normoxic condition followed by 24 hrs incubation under hypoxic condition by HRE-luciferase reporter gene assay
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Examining the structure-activity relationship of benzopyran-based inhibitors of the hypoxia inducible factor-1 pathway.
Ferguson J, De Los Santos Z, Devi N, Van Meir E, Zingales S, Wang B.
Bioorg Med Chem Lett (2017) 27 : 1731 -1736
PubMed 28285917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.80 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099674 — — 1 6.60
CHEMBL1940227 — — 1 6.55
CHEMBL4070128 — — 1 6.41
CHEMBL1940040 — — 1 6.30
CHEMBL1823895 — — 1 6.23
CHEMBL4067812 — — 1 6.12
CHEMBL4059951 — — 1 6.01
CHEMBL4080730 — — 1 6.00
CHEMBL4087304 — — 1 6.00
CHEMBL4072788 — — 1 5.92
CHEMBL4098773 — — 1 5.89
CHEMBL4075842 — — 1 5.82
CHEMBL4101907 — — 1 5.75
CHEMBL4089729 — — 1 5.75
CHEMBL4061391 — — 1 5.60
CHEMBL4099744 — — 1 5.52
CHEMBL4068610 — — 1 5.51
CHEMBL4089700 — — 1 5.50
CHEMBL4081868 — — 1 5.50
CHEMBL4099987 — — 1 5.48
CHEMBL4070062 — — 1 5.46
CHEMBL4083179 — — 1 5.41
CHEMBL4083242 — — 1 5.40
CHEMBL4061468 — — 1 5.40
CHEMBL4065979 — — 1 5.36
CHEMBL4086543 — — 1 5.34
CHEMBL4075824 — — 1 -
CHEMBL4060365 — — 1 -
CHEMBL4088599 — — 1 -
CHEMBL4087625 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099674 — IC50 = 250.0 nM 6.60
CHEMBL1940227 — IC50 = 280.0 nM 6.55
CHEMBL4070128 — IC50 = 390.0 nM 6.41
CHEMBL1940040 — IC50 = 500.0 nM 6.30
CHEMBL1823895 — IC50 = 590.0 nM 6.23
CHEMBL4067812 — IC50 = 750.0 nM 6.12
CHEMBL4059951 — IC50 = 980.0 nM 6.01
CHEMBL4080730 — IC50 = 1000.0 nM 6.00
CHEMBL4087304 — IC50 = 1000.0 nM 6.00
CHEMBL4072788 — IC50 = 1200.0 nM 5.92
CHEMBL4098773 — IC50 = 1300.0 nM 5.89
CHEMBL4075842 — IC50 = 1500.0 nM 5.82
CHEMBL4101907 — IC50 = 1800.0 nM 5.75
CHEMBL4089729 — IC50 = 1800.0 nM 5.75
CHEMBL4061391 — IC50 = 2500.0 nM 5.60
CHEMBL4099744 — IC50 = 3000.0 nM 5.52
CHEMBL4068610 — IC50 = 3100.0 nM 5.51
CHEMBL4089700 — IC50 = 3200.0 nM 5.50
CHEMBL4081868 — IC50 = 3200.0 nM 5.50
CHEMBL4099987 — IC50 = 3300.0 nM 5.48
CHEMBL4070062 — IC50 = 3500.0 nM 5.46
CHEMBL4083179 — IC50 = 3900.0 nM 5.41
CHEMBL4061468 — IC50 = 4000.0 nM 5.40
CHEMBL4083242 — IC50 = 4000.0 nM 5.40
CHEMBL4065979 — IC50 = 4400.0 nM 5.36
CHEMBL4086543 — IC50 = 4600.0 nM 5.34
CHEMBL4079424 — IC50 > 5000.0 nM -
CHEMBL4097457 — IC50 > 5000.0 nM -
CHEMBL4071445 — IC50 > 5000.0 nM -
CHEMBL4105161 — IC50 > 5000.0 nM -
CHEMBL4094061 — IC50 > 5000.0 nM -
CHEMBL4076360 — IC50 > 5000.0 nM -
CHEMBL4094306 — IC50 > 5000.0 nM -
CHEMBL4104442 — IC50 > 5000.0 nM -
CHEMBL4072859 — IC50 > 5000.0 nM -
CHEMBL4091090 — IC50 > 5000.0 nM -
CHEMBL4098836 — IC50 > 5000.0 nM -
CHEMBL4060439 — IC50 > 5000.0 nM -
CHEMBL4087625 — IC50 > 5000.0 nM -
CHEMBL4088599 — IC50 > 5000.0 nM -
CHEMBL4060365 — IC50 > 5000.0 nM -
CHEMBL4075824 — IC50 > 5000.0 nM -