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Assay Detail

CHEMBL698033

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

Binding
Reversible inhibition of recombinant human IL-1 beta converting enzyme.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1-CONVERTING ENZYME (ICE)
Semple G, Ashworth DM, Baker GR, Batt AR, Baxter AJ, Benzies DW, Elliot LH, Evans D, Franklin RJ, Hudson P, Jenkins PD, Pitt GR, Rooker DP, Sheppard A, Szelke M, Yamamoto S, Isomura Y
Bioorg Med Chem Lett (1997) 7 : 1337 -1342
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.86 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286519 1 9.82
CHEMBL26544 1 9.82
CHEMBL553107 1 9.70
CHEMBL2371932 1 8.96
CHEMBL25943 1 8.89
CHEMBL25925 1 8.85
CHEMBL287440 1 8.82
CHEMBL284219 1 8.74
CHEMBL26719 1 8.74
CHEMBL26359 1 8.70
CHEMBL26413 1 8.66
CHEMBL282198 1 8.28
CHEMBL418573 1 8.15
CHEMBL26088 1 8.15
CHEMBL25864 1 8.00
CHEMBL284415 1 7.85
CHEMBL280794 1 7.80
CHEMBL27304 1 7.68
CHEMBL444034 1 7.60
CHEMBL282408 1 7.41
CHEMBL26302 1 7.40
CHEMBL287020 1 7.40
CHEMBL422400 1 7.35
CHEMBL281953 1 7.34
CHEMBL281168 1 7.18
CHEMBL26916 1 7.17
CHEMBL283694 1 7.02
CHEMBL28400 1 6.80
CHEMBL27430 1 6.28
CHEMBL26377 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286519 Ki = 0.15 nM 9.82
CHEMBL26544 Ki = 0.15 nM 9.82
CHEMBL553107 Ki = 0.2 nM 9.70
CHEMBL2371932 Ki = 1.1 nM 8.96
CHEMBL25943 Ki = 1.3 nM 8.89
CHEMBL25925 Ki = 1.4 nM 8.85
CHEMBL287440 Ki = 1.5 nM 8.82
CHEMBL284219 Ki = 1.8 nM 8.74
CHEMBL26719 Ki = 1.8 nM 8.74
CHEMBL26359 Ki = 2.0 nM 8.70
CHEMBL26413 Ki = 2.2 nM 8.66
CHEMBL282198 Ki = 5.3 nM 8.28
CHEMBL418573 Ki = 7.0 nM 8.15
CHEMBL26088 Ki = 7.1 nM 8.15
CHEMBL25864 Ki = 10.0 nM 8.00
CHEMBL284415 Ki = 14.0 nM 7.85
CHEMBL280794 Ki = 16.0 nM 7.80
CHEMBL27304 Ki = 21.0 nM 7.68
CHEMBL444034 Ki = 25.0 nM 7.60
CHEMBL282408 Ki = 39.0 nM 7.41
CHEMBL26302 Ki = 40.0 nM 7.40
CHEMBL287020 Ki = 40.0 nM 7.40
CHEMBL422400 Ki = 45.0 nM 7.35
CHEMBL281953 Ki = 46.0 nM 7.34
CHEMBL281168 Ki = 66.0 nM 7.18
CHEMBL26916 Ki = 68.0 nM 7.17
CHEMBL283694 Ki = 95.0 nM 7.02
CHEMBL28400 Ki = 160.0 nM 6.80
CHEMBL27430 Ki = 530.0 nM 6.28
CHEMBL26377 Ki = 590.0 nM 6.23
CHEMBL285320 Ki = 2200.0 nM 5.66
CHEMBL26027 Ki = 7200.0 nM 5.14