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Assay Detail

CHEMBL4411721

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

Binding
Inhibition of PHD (unknown origin) expressed in mouse NIH/3T3 cells harboring HRE-driven luciferase gene assessed as transactivation of HIF1alpha after 6 hrs by luciferase reporter gene assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Hypoxia-inducible factor prolyl hydroxylase (CHEMBL3831261)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Triterpenoid Hydroxamates as HIF Prolyl Hydrolase Inhibitors.
Minassi A, Rogati F, Cruz C, Prados ME, Galera N, Jinénez C, Appendino G, Bellido ML, Calzado MA, Caprioglio D, Muñoz E.
J Nat Prod (2018) 81 : 2235 -2243
PubMed 30350996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.24 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4463388 1 5.62
CHEMBL4464252 1 5.58
CHEMBL4459542 1 5.50
CHEMBL4519581 1 5.42
CHEMBL4514184 1 5.32
CHEMBL4589866 1 5.30
CHEMBL4472548 1 5.24
CHEMBL4583726 1 5.17
CHEMBL4563191 1 5.15
CHEMBL4592450 1 5.12
CHEMBL3753400 1 5.11
CHEMBL4436329 1 5.05
CHEMBL4562991 1 4.94
CHEMBL3754102 1 4.79
CHEMBL1271303 1 -
CHEMBL4064111 1 -
CHEMBL230006 ENOXOLONE 2.0 1 -
CHEMBL201515 MASLINIC ACID 1 -
CHEMBL269277 BETULINIC ACID 1.0 1 -
CHEMBL169 URSOLIC ACID 2.0 1 -
CHEMBL168 OLEANOLIC_ACID 1 -
CHEMBL4460360 1 -
CHEMBL4473530 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4463388 EC50 = 2400.0 nM 5.62
CHEMBL4464252 EC50 = 2600.0 nM 5.58
CHEMBL4459542 EC50 = 3200.0 nM 5.50
CHEMBL4519581 EC50 = 3800.0 nM 5.42
CHEMBL4514184 EC50 = 4800.0 nM 5.32
CHEMBL4589866 EC50 = 5000.0 nM 5.30
CHEMBL4472548 EC50 = 5800.0 nM 5.24
CHEMBL4583726 EC50 = 6800.0 nM 5.17
CHEMBL4563191 EC50 = 7100.0 nM 5.15
CHEMBL4592450 EC50 = 7500.0 nM 5.12
CHEMBL3753400 EC50 = 7700.0 nM 5.11
CHEMBL4436329 EC50 = 8900.0 nM 5.05
CHEMBL4562991 EC50 = 11400.0 nM 4.94
CHEMBL3754102 EC50 = 16400.0 nM 4.79
CHEMBL1271303 EC50 > 50000.0 nM -
CHEMBL4064111 EC50 > 50000.0 nM -
CHEMBL230006 ENOXOLONE EC50 > 50000.0 nM -
CHEMBL201515 MASLINIC ACID EC50 > 50000.0 nM -
CHEMBL269277 BETULINIC ACID EC50 > 50000.0 nM -
CHEMBL169 URSOLIC ACID EC50 > 50000.0 nM -
CHEMBL168 OLEANOLIC_ACID EC50 > 50000.0 nM -
CHEMBL4460360 EC50 > 50000.0 nM -
CHEMBL4473530 EC50 > 50000.0 nM -