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Assay Detail

CHEMBL1227797

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Binding
Inhibition of human ICE
ChEMBL ↗
56
Total Activities
28
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Caspase-1 (CHEMBL4801) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).
Galatsis P, Caprathe B, Gilmore J, Thomas A, Linn K, Sheehan S, Harter W, Kostlan C, Lunney E, Stankovic C, Rubin J, Brady K, Allen H, Talanian R.
Bioorg Med Chem Lett (2010) 20 : 5184 -5190
PubMed 20656488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.19 9.24
IC50 28 7.38 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1221597 — — 2 9.24
CHEMBL437105 VRT-18858 -1.0 2 9.22
CHEMBL37630 — — 2 9.15
CHEMBL1221644 — — 2 9.05
CHEMBL1221595 — — 2 9.02
CHEMBL1221691 — — 2 8.90
CHEMBL1221643 — — 2 8.89
CHEMBL1221743 — — 2 8.88
CHEMBL1221745 — — 2 8.74
CHEMBL1221688 — — 2 8.55
CHEMBL1221744 — — 2 8.52
CHEMBL1221690 — — 2 8.41
CHEMBL1221645 — — 2 8.39
CHEMBL1221811 — — 2 8.37
CHEMBL1221689 — — 2 8.33
CHEMBL1221647 — — 2 8.31
CHEMBL1221598 — — 2 8.30
CHEMBL1221599 — — 2 8.10
CHEMBL1221549 — — 2 8.03
CHEMBL1221746 — — 2 7.78
CHEMBL1221547 — — 2 7.77
CHEMBL1221646 — — 2 7.70
CHEMBL1221550 — — 2 7.67
CHEMBL1221503 — — 2 7.15
CHEMBL1221548 — — 2 7.00
CHEMBL1221502 — — 2 6.94
CHEMBL1221546 — — 2 6.93
CHEMBL1221596 — — 2 5.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1221597 — Ki = 0.58 nM 9.24
CHEMBL437105 VRT-18858 Ki = 0.6 nM 9.22
CHEMBL37630 — Ki = 0.7 nM 9.15
CHEMBL1221644 — Ki = 0.9 nM 9.05
CHEMBL1221595 — Ki = 0.95 nM 9.02
CHEMBL1221691 — Ki = 1.26 nM 8.90
CHEMBL1221643 — Ki = 1.29 nM 8.89
CHEMBL1221743 — Ki = 1.31 nM 8.88
CHEMBL1221745 — Ki = 1.81 nM 8.74
CHEMBL1221688 — Ki = 2.81 nM 8.55
CHEMBL1221744 — Ki = 3.0 nM 8.52
CHEMBL437105 VRT-18858 IC50 = 3.4 nM 8.47
CHEMBL1221744 — IC50 = 3.61 nM 8.44
CHEMBL1221690 — Ki = 3.85 nM 8.41
CHEMBL1221645 — Ki = 4.03 nM 8.39
CHEMBL1221811 — Ki = 4.3 nM 8.37
CHEMBL1221689 — Ki = 4.68 nM 8.33
CHEMBL1221743 — IC50 = 4.77 nM 8.32
CHEMBL1221647 — Ki = 4.85 nM 8.31
CHEMBL1221598 — Ki = 5.02 nM 8.30
CHEMBL1221597 — IC50 = 5.7 nM 8.24
CHEMBL1221745 — IC50 = 5.81 nM 8.24
CHEMBL1221599 — Ki = 7.9 nM 8.10
CHEMBL1221691 — IC50 = 9.18 nM 8.04
CHEMBL1221549 — Ki = 9.24 nM 8.03
CHEMBL1221595 — IC50 = 11.2 nM 7.95
CHEMBL1221811 — IC50 = 12.0 nM 7.92
CHEMBL1221688 — IC50 = 14.5 nM 7.84
CHEMBL1221647 — IC50 = 15.3 nM 7.82
CHEMBL1221746 — Ki = 16.7 nM 7.78
CHEMBL37630 — IC50 = 17.0 nM 7.77
CHEMBL1221547 — Ki = 16.9 nM 7.77
CHEMBL1221643 — IC50 = 18.0 nM 7.75
CHEMBL1221646 — Ki = 20.0 nM 7.70
CHEMBL1221550 — Ki = 21.5 nM 7.67
CHEMBL1221598 — IC50 = 23.1 nM 7.64
CHEMBL1221689 — IC50 = 23.8 nM 7.62
CHEMBL1221690 — IC50 = 26.5 nM 7.58
CHEMBL1221646 — IC50 = 33.7 nM 7.47
CHEMBL1221599 — IC50 = 37.0 nM 7.43
CHEMBL1221644 — IC50 = 42.5 nM 7.37
CHEMBL1221645 — IC50 = 45.3 nM 7.34
CHEMBL1221503 — Ki = 70.9 nM 7.15
CHEMBL1221548 — Ki = 100.0 nM 7.00
CHEMBL1221746 — IC50 = 102.0 nM 6.99
CHEMBL1221549 — IC50 = 114.0 nM 6.94
CHEMBL1221502 — Ki = 115.0 nM 6.94
CHEMBL1221546 — Ki = 118.0 nM 6.93
CHEMBL1221550 — IC50 = 170.0 nM 6.77
CHEMBL1221546 — IC50 = 398.0 nM 6.40