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Assay Detail

CHEMBL5738965

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Binding
EnPlex (purified enzyme activity assay): This assay is described in Bachovchin et al. Nature Chemical Biology 10, 656-663 (2014). Briefly, purified enzymes are coupled to Luminex microspheres, with a different bead color for each enzyme. Multiplexed bead complexes are incubated with a compound before being treated with a biotinylated activity-based probe and a streptavidin R-phycoerythrin conjugate (SAPE). The mixtures are scanned on a Luminex flow cytometer, where one laser detects the bead color (enzyme identity) and a second laser detects the R-phycoerythrin signal (enzyme activity). The enzyme concentration is calculated assuming 100% of the protein was coupled to the beads.
ChEMBL ↗
144
Total Activities
47
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists
(2023)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 6.29 7.82
kon 48 - -
k_off 48 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6020304 — — 3 7.82
CHEMBL6004569 — — 3 7.64
CHEMBL63406 — — 3 7.62
CHEMBL3686737 — — 3 7.52
CHEMBL5981431 — — 3 7.47
CHEMBL67279 TALABOSTAT 3.0 3 7.46
CHEMBL6059875 — — 3 7.38
CHEMBL5957037 — — 3 7.31
CHEMBL5925037 — — 3 7.24
CHEMBL1790483 — — 3 7.24
CHEMBL5968328 — — 3 7.17
CHEMBL63652 — — 3 7.15
CHEMBL5824868 — — 3 6.80
CHEMBL5809136 — — 3 6.70
CHEMBL63860 — — 6 6.62
CHEMBL494497 — — 3 6.47
CHEMBL66032 — — 3 6.42
CHEMBL63726 — — 3 6.38
CHEMBL63895 — — 3 6.38
CHEMBL5925489 — — 3 6.36
CHEMBL3686733 — — 3 6.36
CHEMBL5817549 — — 3 6.14
CHEMBL6055810 — — 3 6.00
CHEMBL63698 — — 3 5.96
CHEMBL5848496 — — 3 5.92
CHEMBL3686736 — — 3 5.89
CHEMBL5778991 — — 3 5.85
CHEMBL5791516 — — 3 5.25
CHEMBL5918829 — — 3 5.00
CHEMBL1814633 — — 3 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6020304 — IC50 = 15.0 nM 7.82
CHEMBL6004569 — IC50 = 23.0 nM 7.64
CHEMBL63406 — IC50 = 24.0 nM 7.62
CHEMBL3686737 — IC50 = 30.0 nM 7.52
CHEMBL5981431 — IC50 = 34.0 nM 7.47
CHEMBL67279 TALABOSTAT IC50 = 35.0 nM 7.46
CHEMBL6059875 — IC50 = 42.0 nM 7.38
CHEMBL5957037 — IC50 = 49.0 nM 7.31
CHEMBL5925037 — IC50 = 58.0 nM 7.24
CHEMBL1790483 — IC50 = 58.0 nM 7.24
CHEMBL5968328 — IC50 = 68.0 nM 7.17
CHEMBL63652 — IC50 = 71.0 nM 7.15
CHEMBL5824868 — IC50 = 160.0 nM 6.80
CHEMBL5809136 — IC50 = 200.0 nM 6.70
CHEMBL63860 — IC50 = 240.0 nM 6.62
CHEMBL63860 — IC50 = 240.0 nM 6.62
CHEMBL494497 — IC50 = 340.0 nM 6.47
CHEMBL66032 — IC50 = 380.0 nM 6.42
CHEMBL63895 — IC50 = 420.0 nM 6.38
CHEMBL63726 — IC50 = 420.0 nM 6.38
CHEMBL3686733 — IC50 = 440.0 nM 6.36
CHEMBL5925489 — IC50 = 441.0 nM 6.36
CHEMBL5817549 — IC50 = 730.0 nM 6.14
CHEMBL6055810 — IC50 = 1000.0 nM 6.00
CHEMBL63698 — IC50 = 1100.0 nM 5.96
CHEMBL5848496 — IC50 = 1200.0 nM 5.92
CHEMBL3686736 — IC50 = 1300.0 nM 5.89
CHEMBL5778991 — IC50 = 1400.0 nM 5.85
CHEMBL5791516 — IC50 = 5569.0 nM 5.25
CHEMBL1814633 — IC50 = 10000.0 nM 5.00
CHEMBL5918829 — IC50 = 10000.0 nM 5.00
CHEMBL5994541 — IC50 = 25120.0 nM 4.60
CHEMBL5846428 — IC50 = 28000.0 nM 4.55
CHEMBL5768759 — IC50 = 87440.0 nM 4.06
CHEMBL6039540 — IC50 = 89450.0 nM 4.05
CHEMBL5804725 — IC50 = 100000.0 nM 4.00
CHEMBL5766821 — kon = - — -
CHEMBL6060914 — k_off = - s-1 -
CHEMBL5766821 — IC50 > 100000.0 nM -
CHEMBL6059646 — k_off = - s-1 -
CHEMBL6059646 — kon = - — -
CHEMBL6059646 — IC50 > 100000.0 nM -
CHEMBL5766821 — k_off = - s-1 -
CHEMBL5768759 — kon = - — -
CHEMBL6060914 — IC50 > 100000.0 nM -
CHEMBL5994541 — kon = - — -
CHEMBL5994541 — k_off = - s-1 -
CHEMBL5846428 — kon = - — -
CHEMBL5817549 — k_off = - s-1 -
CHEMBL5791516 — kon = - — -