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Assay Detail

CHEMBL864541

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Binding
Inhibitory activity against porcine calpain I using Suc-Leu-Tyr-AMC fluorogenic substrate
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL4062) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.
Lescop C, Herzner H, Siendt H, Bolliger R, Henneböhle M, Weyermann P, Briguet A, Courdier-Fruh I, Erb M, Foster M, Meier T, Magyar JP, von Sprecher A.
Bioorg Med Chem Lett (2005) 15 : 5176 -5181
PubMed 16185867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 7.06 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201987 — — 1 7.70
CHEMBL200826 — — 1 7.70
CHEMBL199007 — — 1 7.70
CHEMBL423112 — — 1 7.70
CHEMBL198620 — — 1 7.62
CHEMBL200254 — — 1 7.52
CHEMBL369951 — — 1 7.41
CHEMBL200468 — — 1 7.40
CHEMBL198480 — — 1 7.30
CHEMBL200283 — — 1 7.22
CHEMBL199758 — — 1 7.22
CHEMBL198962 — — 1 7.22
CHEMBL372348 — — 1 7.16
CHEMBL371038 — — 1 7.16
CHEMBL198587 — — 1 7.10
CHEMBL191881 LEUPEPTIN — 1 7.10
CHEMBL371892 — — 1 7.10
CHEMBL424668 — — 1 7.10
CHEMBL426828 — — 1 7.05
CHEMBL370597 — — 1 7.00
CHEMBL200430 — — 1 7.00
CHEMBL370553 — — 1 7.00
CHEMBL263829 — — 1 7.00
CHEMBL371773 — — 1 7.00
CHEMBL200784 — — 1 7.00
CHEMBL200402 — — 1 7.00
CHEMBL198636 — — 1 7.00
CHEMBL198638 — — 1 7.00
CHEMBL197060 — — 1 7.00
CHEMBL370163 — — 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201987 — IC50 = 20.0 nM 7.70
CHEMBL200826 — IC50 = 20.0 nM 7.70
CHEMBL199007 — IC50 = 20.0 nM 7.70
CHEMBL423112 — IC50 = 20.0 nM 7.70
CHEMBL198620 — IC50 = 24.0 nM 7.62
CHEMBL200254 — IC50 = 30.0 nM 7.52
CHEMBL369951 — IC50 = 39.0 nM 7.41
CHEMBL200468 — IC50 = 40.0 nM 7.40
CHEMBL198480 — IC50 = 50.0 nM 7.30
CHEMBL200283 — IC50 = 60.0 nM 7.22
CHEMBL199758 — IC50 = 60.0 nM 7.22
CHEMBL198962 — IC50 = 60.0 nM 7.22
CHEMBL372348 — IC50 = 70.0 nM 7.16
CHEMBL371038 — IC50 = 70.0 nM 7.16
CHEMBL424668 — IC50 = 80.0 nM 7.10
CHEMBL198587 — IC50 = 80.0 nM 7.10
CHEMBL371892 — IC50 = 80.0 nM 7.10
CHEMBL191881 LEUPEPTIN IC50 = 80.0 nM 7.10
CHEMBL426828 — IC50 = 90.0 nM 7.05
CHEMBL197060 — IC50 = 100.0 nM 7.00
CHEMBL198638 — IC50 = 100.0 nM 7.00
CHEMBL198636 — IC50 = 100.0 nM 7.00
CHEMBL200402 — IC50 = 100.0 nM 7.00
CHEMBL200784 — IC50 = 100.0 nM 7.00
CHEMBL263829 — IC50 = 100.0 nM 7.00
CHEMBL370553 — IC50 = 100.0 nM 7.00
CHEMBL200430 — IC50 = 100.0 nM 7.00
CHEMBL370597 — IC50 = 100.0 nM 7.00
CHEMBL371773 — IC50 = 100.0 nM 7.00
CHEMBL370163 — IC50 = 120.0 nM 6.92
CHEMBL381417 — IC50 = 120.0 nM 6.92
CHEMBL200419 — IC50 = 120.0 nM 6.92
CHEMBL200604 — IC50 = 120.0 nM 6.92
CHEMBL200872 — IC50 = 150.0 nM 6.82
CHEMBL199482 — IC50 = 150.0 nM 6.82
CHEMBL371772 — IC50 = 180.0 nM 6.75
CHEMBL200645 — IC50 = 200.0 nM 6.70
CHEMBL195183 — IC50 = 230.0 nM 6.64
CHEMBL200096 — IC50 = 250.0 nM 6.60
CHEMBL200603 — IC50 = 400.0 nM 6.40
CHEMBL197438 — IC50 = 400.0 nM 6.40
CHEMBL200147 — IC50 = 500.0 nM 6.30
CHEMBL373191 — IC50 > 1000.0 nM -
CHEMBL200307 — IC50 > 1000.0 nM -
CHEMBL370610 — IC50 > 1000.0 nM -
CHEMBL200873 — IC50 > 1000.0 nM -
CHEMBL197476 — IC50 > 1000.0 nM -
CHEMBL197018 — IC50 > 10000.0 nM -
CHEMBL198539 — IC50 > 1000.0 nM -
CHEMBL435932 — IC50 > 1000.0 nM -