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Assay Detail

CHEMBL4050596

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

Binding
Inhibition of recombinant human PACE4 expressed in drosophila S2 cells using pyrGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin as substrate after 60 mins by spectrofluorometry method
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proprotein convertase subtilisin/kexin type 6 (CHEMBL2951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Positional Scanning Identifies the Molecular Determinants of a High Affinity Multi-Leucine Inhibitor for Furin and PACE4.
Małuch I, Levesque C, Kwiatkowska A, Couture F, Ly K, Desjardins R, Neugebauer WA, Prahl A, Day R.
J Med Chem (2017) 60 : 2732 -2744
PubMed 28287731 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 75 8.30 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4089819 1 9.70
CHEMBL4065072 1 9.52
CHEMBL4084457 1 9.40
CHEMBL4091099 1 9.40
CHEMBL4100996 1 9.30
CHEMBL4104777 1 9.22
CHEMBL4070237 1 9.05
CHEMBL4064275 1 9.00
CHEMBL4083310 1 9.00
CHEMBL4073661 1 8.89
CHEMBL4094478 1 8.82
CHEMBL4099961 1 8.77
CHEMBL4097940 1 8.74
CHEMBL4093570 1 8.70
CHEMBL4063327 1 8.70
CHEMBL4096348 1 8.70
CHEMBL4101342 1 8.70
CHEMBL4103443 1 8.70
CHEMBL4087970 1 8.70
CHEMBL4085824 1 8.70
CHEMBL4075692 1 8.68
CHEMBL4072949 1 8.66
CHEMBL4065627 1 8.60
CHEMBL4084913 1 8.55
CHEMBL4059801 1 8.55
CHEMBL4067772 1 8.52
CHEMBL4063219 1 8.52
CHEMBL4089913 1 8.52
CHEMBL4080551 1 8.52
CHEMBL4093266 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4089819 Ki = 0.2 nM 9.70
CHEMBL4065072 Ki = 0.3 nM 9.52
CHEMBL4084457 Ki = 0.4 nM 9.40
CHEMBL4091099 Ki = 0.4 nM 9.40
CHEMBL4100996 Ki = 0.5 nM 9.30
CHEMBL4104777 Ki = 0.6 nM 9.22
CHEMBL4070237 Ki = 0.9 nM 9.05
CHEMBL4064275 Ki = 1.0 nM 9.00
CHEMBL4083310 Ki = 1.0 nM 9.00
CHEMBL4073661 Ki = 1.3 nM 8.89
CHEMBL4094478 Ki = 1.5 nM 8.82
CHEMBL4099961 Ki = 1.7 nM 8.77
CHEMBL4097940 Ki = 1.8 nM 8.74
CHEMBL4087970 Ki = 2.0 nM 8.70
CHEMBL4063327 Ki = 2.0 nM 8.70
CHEMBL4096348 Ki = 2.0 nM 8.70
CHEMBL4101342 Ki = 2.0 nM 8.70
CHEMBL4103443 Ki = 2.0 nM 8.70
CHEMBL4093570 Ki = 2.0 nM 8.70
CHEMBL4085824 Ki = 2.0 nM 8.70
CHEMBL4075692 Ki = 2.1 nM 8.68
CHEMBL4072949 Ki = 2.2 nM 8.66
CHEMBL4065627 Ki = 2.5 nM 8.60
CHEMBL4084913 Ki = 2.8 nM 8.55
CHEMBL4059801 Ki = 2.8 nM 8.55
CHEMBL4067772 Ki = 3.0 nM 8.52
CHEMBL4093266 Ki = 3.0 nM 8.52
CHEMBL4080551 Ki = 3.0 nM 8.52
CHEMBL4063219 Ki = 3.0 nM 8.52
CHEMBL4089913 Ki = 3.0 nM 8.52
CHEMBL4076965 Ki = 3.7 nM 8.43
CHEMBL4063459 Ki = 4.0 nM 8.40
CHEMBL4066994 Ki = 4.0 nM 8.40
CHEMBL4060537 Ki = 4.0 nM 8.40
CHEMBL4101304 Ki = 4.0 nM 8.40
CHEMBL4092088 Ki = 4.0 nM 8.40
CHEMBL4077533 Ki = 4.0 nM 8.40
CHEMBL4097058 Ki = 4.0 nM 8.40
CHEMBL4091172 Ki = 4.1 nM 8.39
CHEMBL4066673 Ki = 4.8 nM 8.32
CHEMBL4103458 Ki = 4.9 nM 8.31
CHEMBL4074250 Ki = 5.0 nM 8.30
CHEMBL4061196 Ki = 5.0 nM 8.30
CHEMBL4094278 Ki = 5.0 nM 8.30
CHEMBL4061737 Ki = 5.0 nM 8.30
CHEMBL4069865 Ki = 6.0 nM 8.22
CHEMBL4068820 Ki = 6.0 nM 8.22
CHEMBL4086512 Ki = 6.0 nM 8.22
CHEMBL4081957 Ki = 6.0 nM 8.22
CHEMBL4099504 Ki = 6.2 nM 8.21