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Assay Detail

CHEMBL5733557

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Binding
In Vitro Assay: TACE:The basis for the assay is the cleavage of the substrate 5FAM-LAQAVRSSSRK-5TAMRA (SEQ ID No 3) (Anaspec, custom 34891) by human TACE (R&D SYSTEMS INC., Cat #930-ADB).For the dose response (10 point), 4 μL of a dilution series of compound (2 mM highest concentration, 1/5 dilution in DMSO further diluted 1 in 10 in water, corresponding to a final highest concentration of 20 μM), is transferred to 384 well Fluotrac 200 plate (Greiner, cat #781076) and incubated at room temperature for 30 min with a 26 μL buffer solution (25 mM Tris pH8.0, 2.5 μM ZnCl2, 0.01% CHAPS) containing TACE (0.05 ng/μL) (it will be appreciated by the skilled person that the potency read out is independent of the enzyme concentration).The reaction is initiated by adding to the assay plate 5FAM-LAQAVRSSSRK-5TAMRA (5 L, 5 μM, Anaspec) in the same buffer.Finally, the fluorescence is read on the Envision (Perkin Elmer) after an incubation of 75 min at room temperature (Excitation 485 nm, Emission 530).
ChEMBL ↗
1299
Total Activities
407
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 433 5.96 7.25
kon 433 - -
k_off 433 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5856297 — — 3 7.25
CHEMBL5962512 — — 6 6.97
CHEMBL6038057 — — 3 6.92
CHEMBL5869212 — — 3 6.87
CHEMBL6061166 — — 3 6.86
CHEMBL4856943 — — 3 6.77
CHEMBL5824315 — — 3 6.71
CHEMBL5746981 — — 3 6.68
CHEMBL5958181 — — 3 6.68
CHEMBL5760423 — — 6 6.65
CHEMBL4846457 — — 6 6.61
CHEMBL6010345 — — 3 6.60
CHEMBL6016907 — — 3 6.57
CHEMBL5753216 — — 3 6.56
CHEMBL5833833 — — 3 6.53
CHEMBL6040418 — — 6 6.51
CHEMBL6036847 — — 3 6.49
CHEMBL5877700 — — 6 6.47
CHEMBL6036531 — — 3 6.46
CHEMBL4868710 — — 3 6.43
CHEMBL5945575 — — 3 6.40
CHEMBL6011623 — — 6 6.38
CHEMBL5940394 — — 3 6.37
CHEMBL6002399 — — 6 6.36
CHEMBL5864715 — — 3 6.34
CHEMBL5866536 — — 3 6.34
CHEMBL4874226 — — 3 6.32
CHEMBL5750841 — — 3 6.32
CHEMBL6039288 — — 3 6.26
CHEMBL5844908 — — 3 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5856297 — IC50 = 56.0 nM 7.25
CHEMBL5962512 — IC50 = 106.0 nM 6.97
CHEMBL5962512 — IC50 = 106.0 nM 6.97
CHEMBL6038057 — IC50 = 120.0 nM 6.92
CHEMBL5869212 — IC50 = 134.0 nM 6.87
CHEMBL6061166 — IC50 = 137.0 nM 6.86
CHEMBL4856943 — IC50 = 170.0 nM 6.77
CHEMBL5824315 — IC50 = 195.0 nM 6.71
CHEMBL5958181 — IC50 = 207.0 nM 6.68
CHEMBL5746981 — IC50 = 211.0 nM 6.68
CHEMBL5760423 — IC50 = 225.0 nM 6.65
CHEMBL5760423 — IC50 = 225.0 nM 6.65
CHEMBL4846457 — IC50 = 245.0 nM 6.61
CHEMBL4846457 — IC50 = 245.0 nM 6.61
CHEMBL6010345 — IC50 = 251.0 nM 6.60
CHEMBL6016907 — IC50 = 272.0 nM 6.57
CHEMBL5753216 — IC50 = 277.0 nM 6.56
CHEMBL5833833 — IC50 = 298.0 nM 6.53
CHEMBL6040418 — IC50 = 311.0 nM 6.51
CHEMBL6040418 — IC50 = 311.0 nM 6.51
CHEMBL6036847 — IC50 = 321.0 nM 6.49
CHEMBL5877700 — IC50 = 337.0 nM 6.47
CHEMBL5877700 — IC50 = 337.0 nM 6.47
CHEMBL6036531 — IC50 = 348.0 nM 6.46
CHEMBL4868710 — IC50 = 368.0 nM 6.43
CHEMBL5945575 — IC50 = 396.0 nM 6.40
CHEMBL6011623 — IC50 = 417.0 nM 6.38
CHEMBL6011623 — IC50 = 417.0 nM 6.38
CHEMBL5940394 — IC50 = 429.0 nM 6.37
CHEMBL6002399 — IC50 = 441.0 nM 6.36
CHEMBL5866536 — IC50 = 461.0 nM 6.34
CHEMBL5864715 — IC50 = 457.0 nM 6.34
CHEMBL4874226 — IC50 = 479.0 nM 6.32
CHEMBL5750841 — IC50 = 479.0 nM 6.32
CHEMBL6039288 — IC50 = 550.0 nM 6.26
CHEMBL5844908 — IC50 = 588.0 nM 6.23
CHEMBL4854306 — IC50 = 670.0 nM 6.17
CHEMBL5777064 — IC50 = 785.0 nM 6.11
CHEMBL6064042 — IC50 = 789.0 nM 6.10
CHEMBL5869494 — IC50 = 787.0 nM 6.10
CHEMBL5909928 — IC50 = 817.0 nM 6.09
CHEMBL5894436 — IC50 = 840.0 nM 6.08
CHEMBL5894436 — IC50 = 840.0 nM 6.08
CHEMBL5904713 — IC50 = 880.0 nM 6.06
CHEMBL5802631 — IC50 = 885.0 nM 6.05
CHEMBL5835240 — IC50 = 963.0 nM 6.02
CHEMBL6051089 — IC50 = 984.0 nM 6.01
CHEMBL5838166 — IC50 = 1000.0 nM 6.00
CHEMBL5923545 — IC50 = 1050.0 nM 5.98
CHEMBL5780086 — IC50 = 1050.0 nM 5.98