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Assay Detail

CHEMBL5737360

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

Binding
TR-Fret Assay: The TR-FRET assay is illustrated in FIG. 3A and FIG. 3B. The TR-FRET assay cocktail was prepared by mixing 50 nM Biotin-DCN1P, 20 nM AlexaFluor488 UBC12 peptide, and 2.5 nM Tb-Streptavidin conjugate (Life Technologies) in 25 mM Hepes, 10 mM NaCl, 0.1% Triton X-100, 0.5 mM DTT, pH 7.5. 20 ul of the cocktail was aliquoted out into black 384-well plates (Corning 8849BC) using the WellMate and incubated for about 1 hour. Compounds were introduced to the desired concentration using the Biomek and the samples were incubated at r.t. for 60 min. The TR-FRET signal was read by the Pherastar plate-reader.
ChEMBL ↗
2070
Total Activities
635
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

DCN1-like protein 1/NEDD8-conjugating enzyme Ubc12 (CHEMBL4523603) ↗
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Methods and compositions of inhibiting DCN1-UBC12 interaction
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 690 5.64 8.37
kon 690 - -
k_off 690 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5908146 — — 3 8.37
CHEMBL5994790 — — 3 8.17
CHEMBL5801181 — — 3 7.75
CHEMBL4077431 — — 3 7.46
CHEMBL4099097 — — 9 7.28
CHEMBL4094517 — — 3 7.25
CHEMBL4077759 — — 3 7.24
CHEMBL4074213 — — 3 7.12
CHEMBL4078685 — — 3 7.12
CHEMBL5955765 — — 3 7.10
CHEMBL4067795 — — 3 7.10
CHEMBL4103209 — — 3 7.09
CHEMBL5892598 — — 3 7.08
CHEMBL4086099 — — 3 7.08
CHEMBL5757781 — — 3 7.07
CHEMBL5909767 — — 3 7.04
CHEMBL5831580 — — 3 7.02
CHEMBL5761495 — — 3 6.96
CHEMBL4102019 — — 9 6.96
CHEMBL5883632 — — 3 6.94
CHEMBL6040893 — — 3 6.94
CHEMBL4077751 — — 6 6.89
CHEMBL6059510 — — 3 6.88
CHEMBL6010509 — — 3 6.85
CHEMBL4229003 — — 6 6.85
CHEMBL5887540 — — 3 6.84
CHEMBL5913381 — — 3 6.81
CHEMBL6050418 — — 3 6.81
CHEMBL4085483 — — 3 6.79
CHEMBL6065716 — — 3 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5908146 — IC50 = 4.3 nM 8.37
CHEMBL5994790 — IC50 = 6.8 nM 8.17
CHEMBL5801181 — IC50 = 18.0 nM 7.75
CHEMBL4077431 — IC50 = 35.0 nM 7.46
CHEMBL4099097 — IC50 = 53.0 nM 7.28
CHEMBL4099097 — IC50 = 53.0 nM 7.28
CHEMBL4094517 — IC50 = 55.9 nM 7.25
CHEMBL4077759 — IC50 = 58.0 nM 7.24
CHEMBL4074213 — IC50 = 76.5 nM 7.12
CHEMBL4078685 — IC50 = 76.7 nM 7.12
CHEMBL5955765 — IC50 = 78.8 nM 7.10
CHEMBL4067795 — IC50 = 78.9 nM 7.10
CHEMBL4103209 — IC50 = 81.8 nM 7.09
CHEMBL4086099 — IC50 = 83.0 nM 7.08
CHEMBL5892598 — IC50 = 82.7 nM 7.08
CHEMBL5757781 — IC50 = 85.3 nM 7.07
CHEMBL4099097 — IC50 = 88.5 nM 7.05
CHEMBL5909767 — IC50 = 90.5 nM 7.04
CHEMBL5831580 — IC50 = 95.1 nM 7.02
CHEMBL5761495 — IC50 = 111.0 nM 6.96
CHEMBL4102019 — IC50 = 110.0 nM 6.96
CHEMBL4102019 — IC50 = 110.0 nM 6.96
CHEMBL6040893 — IC50 = 116.0 nM 6.94
CHEMBL5883632 — IC50 = 116.0 nM 6.94
CHEMBL4102019 — IC50 = 119.0 nM 6.92
CHEMBL4077751 — IC50 = 130.0 nM 6.89
CHEMBL6059510 — IC50 = 131.0 nM 6.88
CHEMBL6010509 — IC50 = 140.0 nM 6.85
CHEMBL4229003 — IC50 = 140.0 nM 6.85
CHEMBL5887540 — IC50 = 143.0 nM 6.84
CHEMBL6050418 — IC50 = 155.0 nM 6.81
CHEMBL5913381 — IC50 = 154.0 nM 6.81
CHEMBL4085483 — IC50 = 163.0 nM 6.79
CHEMBL6065716 — IC50 = 165.0 nM 6.78
CHEMBL4103413 — IC50 = 166.0 nM 6.78
CHEMBL4440896 — IC50 = 172.0 nM 6.76
CHEMBL4225246 — IC50 = 178.0 nM 6.75
CHEMBL4225246 — IC50 = 180.0 nM 6.75
CHEMBL5819269 — IC50 = 184.0 nM 6.74
CHEMBL4072130 — IC50 = 190.0 nM 6.72
CHEMBL5835337 — IC50 = 190.0 nM 6.72
CHEMBL4077301 — IC50 = 202.0 nM 6.70
CHEMBL4093853 — IC50 = 200.0 nM 6.70
CHEMBL4072130 — IC50 = 201.0 nM 6.70
CHEMBL6057566 — IC50 = 206.0 nM 6.69
CHEMBL4229003 — IC50 = 207.0 nM 6.68
CHEMBL5839127 — IC50 = 208.0 nM 6.68
CHEMBL5980233 — IC50 = 213.0 nM 6.67
CHEMBL5941186 — IC50 = 227.0 nM 6.64
CHEMBL4064579 — IC50 = 237.0 nM 6.62