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Assay Detail

CHEMBL3223500

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

Binding
Inhibition of HIF-1 (unknown origin) expressed in human HeLa cells after 12 hrs by HRE luciferase reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity
Takeuchi A, Hori M, Sato S, Ban HS, Kuchimaru T, Kizaka-Kondoh S, Yamori T, Nakamura H
Medchemcomm (2012) 3 : 1455 -1461
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.06 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220252 1 7.16
CHEMBL434085 1 7.00
CHEMBL3220253 1 6.75
CHEMBL164712 1 6.58
CHEMBL3220249 1 6.57
CHEMBL164448 1 6.52
CHEMBL3220251 1 6.51
CHEMBL164379 1 6.34
CHEMBL353853 1 6.32
CHEMBL350349 1 6.28
CHEMBL3220258 1 6.21
CHEMBL3220254 1 6.19
CHEMBL3220257 1 6.16
CHEMBL3220256 1 6.08
CHEMBL3220250 1 6.01
CHEMBL202258 1 5.91
CHEMBL333985 1 5.70
CHEMBL3220255 1 5.55
CHEMBL3220246 1 5.48
CHEMBL3220259 1 5.16
CHEMBL3220245 1 5.05
CHEMBL3220248 1 5.03
CHEMBL3220247 1 4.86
CHEMBL3220260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220252 IC50 = 70.0 nM 7.16
CHEMBL434085 IC50 = 100.0 nM 7.00
CHEMBL3220253 IC50 = 180.0 nM 6.75
CHEMBL164712 IC50 = 260.0 nM 6.58
CHEMBL3220249 IC50 = 270.0 nM 6.57
CHEMBL164448 IC50 = 300.0 nM 6.52
CHEMBL3220251 IC50 = 310.0 nM 6.51
CHEMBL164379 IC50 = 460.0 nM 6.34
CHEMBL353853 IC50 = 480.0 nM 6.32
CHEMBL350349 IC50 = 530.0 nM 6.28
CHEMBL3220258 IC50 = 610.0 nM 6.21
CHEMBL3220254 IC50 = 650.0 nM 6.19
CHEMBL3220257 IC50 = 700.0 nM 6.16
CHEMBL3220256 IC50 = 830.0 nM 6.08
CHEMBL3220250 IC50 = 970.0 nM 6.01
CHEMBL202258 IC50 = 1240.0 nM 5.91
CHEMBL333985 IC50 = 2000.0 nM 5.70
CHEMBL3220255 IC50 = 2800.0 nM 5.55
CHEMBL3220246 IC50 = 3300.0 nM 5.48
CHEMBL3220259 IC50 = 7000.0 nM 5.16
CHEMBL3220245 IC50 = 9000.0 nM 5.05
CHEMBL3220248 IC50 = 9400.0 nM 5.03
CHEMBL3220247 IC50 = 13900.0 nM 4.86
CHEMBL3220260 IC50 > 30000.0 nM -