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Assay Detail

CHEMBL3705266

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

Binding
Spectrophotometic Assay: Spectrophotometic Assay: This novel assay was used to determine the kinetic parameters for most of the QC substrates. QC activity was analyzed spectrophotometrically using a continuous method, that was derived by adapting a previous discontinuous assay (Bateman, R.C.J. 1989 J Neurosci Methods 30, 23-28).
ChEMBL ↗
195
Total Activities
184
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutaminyl-peptide cyclotransferase (CHEMBL4508) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 185 6.32 6.80
Ki 10 7.10 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3659481 — — 2 7.90
CHEMBL3659480 — — 2 7.47
CHEMBL3659477 VAROGLUTAMSTAT 2.0 2 7.43
CHEMBL3985410 — — 2 7.39
CHEMBL3659482 — — 2 7.27
CHEMBL3659483 — — 2 7.23
CHEMBL3659475 — — 2 7.20
CHEMBL3659478 — — 2 7.12
CHEMBL3659479 — — 2 6.83
CHEMBL3659476 — — 2 5.14
CHEMBL3985594 — — 1 -
CHEMBL3956928 — — 1 -
CHEMBL3896797 — — 1 -
CHEMBL3943360 — — 1 -
CHEMBL3890714 — — 1 -
CHEMBL3917896 — — 1 -
CHEMBL3948264 — — 1 -
CHEMBL3889887 — — 1 -
CHEMBL3917897 — — 1 -
CHEMBL3902400 — — 1 -
CHEMBL3908189 — — 1 -
CHEMBL3905042 — — 1 -
CHEMBL3975820 — — 1 -
CHEMBL3891466 — — 1 -
CHEMBL3928442 — — 1 -
CHEMBL3898159 — — 1 -
CHEMBL4107671 — — 1 -
CHEMBL3917999 — — 2 -
CHEMBL3922519 — — 1 -
CHEMBL3896789 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3659481 — Ki = 12.5 nM 7.90
CHEMBL3659480 — Ki = 33.6 nM 7.47
CHEMBL3659477 VAROGLUTAMSTAT Ki = 37.4 nM 7.43
CHEMBL3985410 — Ki = 40.8 nM 7.39
CHEMBL3659482 — Ki = 53.5 nM 7.27
CHEMBL3659483 — Ki = 58.8 nM 7.23
CHEMBL3659475 — Ki = 62.5 nM 7.20
CHEMBL3659478 — Ki = 75.0 nM 7.12
CHEMBL3659479 — Ki = 149.0 nM 6.83
CHEMBL3659481 — IC50 = 160.0 nM 6.80
CHEMBL3659480 — IC50 = 170.0 nM 6.77
CHEMBL3659477 VAROGLUTAMSTAT IC50 = 238.0 nM 6.62
CHEMBL3659483 — IC50 = 240.0 nM 6.62
CHEMBL3985410 — IC50 = 254.0 nM 6.59
CHEMBL3659482 — IC50 = 297.0 nM 6.53
CHEMBL3659478 — IC50 = 397.0 nM 6.40
CHEMBL3659475 — IC50 = 482.0 nM 6.32
CHEMBL3659479 — IC50 = 882.0 nM 6.05
CHEMBL3659476 — Ki = 7250.0 nM 5.14
CHEMBL3659476 — IC50 = 30200.0 nM 4.52
CHEMBL3968625 — IC50 < 10000.0 nM -
CHEMBL3977130 — IC50 < 10000.0 nM -
CHEMBL3900219 — IC50 < 10000.0 nM -
CHEMBL3974634 — IC50 < 10000.0 nM -
CHEMBL3910437 — IC50 < 10000.0 nM -
CHEMBL4110225 — IC50 < 10000.0 nM -
CHEMBL3919365 — IC50 < 10000.0 nM -
CHEMBL3960005 — IC50 < 10000.0 nM -
CHEMBL3895472 — IC50 < 10000.0 nM -
CHEMBL3923461 — IC50 < 10000.0 nM -
CHEMBL3922411 — IC50 < 10000.0 nM -
CHEMBL3909980 — IC50 < 10000.0 nM -
CHEMBL3937918 — IC50 < 10000.0 nM -
CHEMBL3985646 — IC50 < 10000.0 nM -
CHEMBL3926755 — IC50 < 10000.0 nM -
CHEMBL3939077 — IC50 < 10000.0 nM -
CHEMBL3910189 — IC50 < 10000.0 nM -
CHEMBL4110411 — IC50 < 10000.0 nM -
CHEMBL3981929 — IC50 < 10000.0 nM -
CHEMBL3964697 — IC50 < 10000.0 nM -
CHEMBL3912068 — IC50 < 10000.0 nM -
CHEMBL4112755 — IC50 < 10000.0 nM -
CHEMBL3913874 — IC50 < 10000.0 nM -
CHEMBL3915587 — IC50 < 10000.0 nM -
CHEMBL4109277 — IC50 < 10000.0 nM -
CHEMBL3904874 — IC50 < 10000.0 nM -
CHEMBL3972294 — IC50 < 10000.0 nM -
CHEMBL3901160 — IC50 < 10000.0 nM -
CHEMBL3924877 — IC50 < 10000.0 nM -
CHEMBL3921966 — IC50 < 10000.0 nM -