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Assay Detail

CHEMBL4809036

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

Functional
Reduction of propionyl-CoA in human hepatocytes derived from propionic acidemia patient pretreated for 30 mins followed by 13C-isoleucine addition and measured after 1 hr by MS/MS analysis
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Hepatocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of 2,2-Dimethylbutanoic Acid (HST5040), a Clinical Development Candidate for the Treatment of Propionic Acidemia and Methylmalonic Acidemia.
Armstrong AJ, Henke BR, Collado MS, Taylor JM, Pourtaheri TD, Dillberger JE, Roper TD, Wamhoff BR, Olson MW, Figler RA, Hoang SA, Reardon JE, Johns BA.
J Med Chem (2021) 64 : 5037 -5048
PubMed 33848153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.15 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4871957 1 6.12
CHEMBL1232385 T-BUTYLACETIC ACID 1 6.04
CHEMBL286013 DIMEBUTIC ACID 2.0 1 6.03
CHEMBL4866386 1 5.91
CHEMBL4873476 1 5.76
CHEMBL4867017 1 5.57
CHEMBL322719 PIVALATE 1 5.26
CHEMBL4868765 1 5.18
CHEMBL4851445 1 5.00
CHEMBL109 VALPROIC ACID 4.0 1 4.93
CHEMBL1902018 1 4.91
CHEMBL1204680 1 4.90
CHEMBL4854573 1 4.81
CHEMBL4866078 1 4.72
CHEMBL4649900 CYCLOPROPANE CARBOXYLIC ACID 1 4.63
CHEMBL184290 1 4.47
CHEMBL1160012 1 4.28
CHEMBL3560137 1 4.26
CHEMBL186602 1 -
CHEMBL170070 1 -
CHEMBL3358702 1 -
CHEMBL4867734 1 -
CHEMBL4861714 1 -
CHEMBL4857473 1 -
CHEMBL4878490 1 -
CHEMBL4865041 1 -
CHEMBL1469 PHENYLBUTANOIC ACID 4.0 1 -
CHEMBL851 PHENYL PROPIONIC ACID 1 -
CHEMBL1044 PHENYLACETIC ACID -1.0 1 -
CHEMBL4873436 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4871957 EC50 = 760.0 nM 6.12
CHEMBL1232385 T-BUTYLACETIC ACID EC50 = 910.0 nM 6.04
CHEMBL286013 DIMEBUTIC ACID EC50 = 940.0 nM 6.03
CHEMBL4866386 EC50 = 1230.0 nM 5.91
CHEMBL4873476 EC50 = 1730.0 nM 5.76
CHEMBL4867017 EC50 = 2690.0 nM 5.57
CHEMBL322719 PIVALATE EC50 = 5530.0 nM 5.26
CHEMBL4868765 EC50 = 6550.0 nM 5.18
CHEMBL4851445 EC50 = 9910.0 nM 5.00
CHEMBL109 VALPROIC ACID EC50 = 11730.0 nM 4.93
CHEMBL1902018 EC50 = 12280.0 nM 4.91
CHEMBL1204680 EC50 = 12590.0 nM 4.90
CHEMBL4854573 EC50 = 15480.0 nM 4.81
CHEMBL4866078 EC50 = 18950.0 nM 4.72
CHEMBL4649900 CYCLOPROPANE CARBOXYLIC ACID EC50 = 23270.0 nM 4.63
CHEMBL184290 EC50 = 33740.0 nM 4.47
CHEMBL1160012 EC50 = 52140.0 nM 4.28
CHEMBL3560137 EC50 = 55370.0 nM 4.26
CHEMBL186602 EC50 > 100000.0 nM -
CHEMBL170070 EC50 > 100000.0 nM -
CHEMBL3358702 EC50 - -
CHEMBL4867734 EC50 - -
CHEMBL4861714 EC50 > 100000.0 nM -
CHEMBL4857473 EC50 - -
CHEMBL4878490 EC50 - -
CHEMBL4865041 EC50 - -
CHEMBL1469 PHENYLBUTANOIC ACID EC50 - -
CHEMBL851 PHENYL PROPIONIC ACID EC50 - -
CHEMBL1044 PHENYLACETIC ACID EC50 - -
CHEMBL4873436 EC50 - -