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Assay Detail

CHEMBL656204

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Binding
Inhibitory activity of alpha-keto esters towards calpain 1 at pH 8.0.
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

Calpain 1 (CHEMBL2111357) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Peptide alpha-keto ester, alpha-keto amide, and alpha-keto acid inhibitors of calpains and other cysteine proteases.
Li Z, Patil GS, Golubski ZE, Hori H, Tehrani K, Foreman JE, Eveleth DD, Bartus RT, Powers JC.
J Med Chem (1993) 36 : 3472 -3480
PubMed 8230139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 6.06 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117023 — — 1 8.07
CHEMBL331850 — — 1 7.28
CHEMBL117840 — — 1 7.16
CHEMBL118908 — — 1 7.12
CHEMBL441280 — — 1 7.10
CHEMBL116429 — — 1 7.02
CHEMBL117776 — — 1 7.00
CHEMBL331322 — — 1 6.92
CHEMBL326290 — — 1 6.80
CHEMBL117336 — — 1 6.70
CHEMBL118025 — — 1 6.70
CHEMBL420872 — — 1 6.70
CHEMBL444594 — — 1 6.70
CHEMBL116894 — — 1 6.68
CHEMBL325147 — — 1 6.60
CHEMBL325401 — — 1 6.55
CHEMBL325223 — — 1 6.50
CHEMBL115701 — — 1 6.50
CHEMBL116256 — — 1 6.50
CHEMBL432443 — — 1 6.30
CHEMBL117888 — — 1 6.17
CHEMBL119622 — — 1 6.10
CHEMBL116746 — — 1 6.00
CHEMBL117255 — — 1 6.00
CHEMBL3142937 — — 1 5.89
CHEMBL117891 — — 1 5.85
CHEMBL3142933 — — 1 5.85
CHEMBL2370490 — — 1 5.75
CHEMBL333388 — — 1 5.75
CHEMBL411658 — — 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117023 — Ki = 8.5 nM 8.07
CHEMBL331850 — Ki = 52.0 nM 7.28
CHEMBL117840 — Ki = 69.0 nM 7.16
CHEMBL118908 — Ki = 75.0 nM 7.12
CHEMBL441280 — Ki = 80.0 nM 7.10
CHEMBL116429 — Ki = 96.0 nM 7.02
CHEMBL117776 — Ki = 100.0 nM 7.00
CHEMBL331322 — Ki = 120.0 nM 6.92
CHEMBL326290 — Ki = 160.0 nM 6.80
CHEMBL117336 — Ki = 200.0 nM 6.70
CHEMBL118025 — Ki = 200.0 nM 6.70
CHEMBL420872 — Ki = 200.0 nM 6.70
CHEMBL444594 — Ki = 200.0 nM 6.70
CHEMBL116894 — Ki = 210.0 nM 6.68
CHEMBL325147 — Ki = 250.0 nM 6.60
CHEMBL325401 — Ki = 280.0 nM 6.55
CHEMBL325223 — Ki = 320.0 nM 6.50
CHEMBL115701 — Ki = 320.0 nM 6.50
CHEMBL116256 — Ki = 320.0 nM 6.50
CHEMBL432443 — Ki = 500.0 nM 6.30
CHEMBL117888 — Ki = 680.0 nM 6.17
CHEMBL119622 — Ki = 800.0 nM 6.10
CHEMBL116746 — Ki = 1000.0 nM 6.00
CHEMBL117255 — Ki = 1000.0 nM 6.00
CHEMBL3142937 — Ki = 1300.0 nM 5.89
CHEMBL3142933 — Ki = 1400.0 nM 5.85
CHEMBL117891 — Ki = 1400.0 nM 5.85
CHEMBL2370490 — Ki = 1800.0 nM 5.75
CHEMBL333388 — Ki = 1800.0 nM 5.75
CHEMBL411658 — Ki = 1800.0 nM 5.75
CHEMBL116458 — Ki = 2000.0 nM 5.70
CHEMBL324834 — Ki = 3400.0 nM 5.47
CHEMBL115757 — Ki = 4000.0 nM 5.40
CHEMBL117905 — Ki = 4500.0 nM 5.35
CHEMBL117450 — Ki = 5000.0 nM 5.30
CHEMBL116358 — Ki = 7000.0 nM 5.16
CHEMBL115630 — Ki = 9500.0 nM 5.02
CHEMBL116477 — Ki = 15000.0 nM 4.82
CHEMBL3142936 — Ki = 16000.0 nM 4.80
CHEMBL331383 — Ki = 20000.0 nM 4.70
CHEMBL3142935 — Ki = 33000.0 nM 4.48
CHEMBL117801 — Ki = 40000.0 nM 4.40
CHEMBL117089 — Ki = 76000.0 nM 4.12
CHEMBL432433 — Ki > 5000.0 nM -
CHEMBL333878 — Ki = - nM -
CHEMBL326725 — Ki = - nM -
CHEMBL117677 — Ki = - nM -
CHEMBL117446 — Ki = - nM -
CHEMBL117232 — Ki < 4000.0 nM -