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Assay Detail

CHEMBL3880449

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

Binding
Inhibition of pig brain TRH-DE using Glp-His-ProAMC as substrate by DPP-4-based continuous fluorometric method
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thyrotropin releasing hormone degrading enzyme (CHEMBL3988623)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

TRH-like peptide derivatives as inhibitors of the TRH-degrading ectoenzyme
(2010)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.09 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3906398 1 6.39
CHEMBL3926920 1 6.07
CHEMBL3915933 1 5.76
CHEMBL3911902 1 5.49
CHEMBL3980061 1 5.18
CHEMBL3921638 1 5.03
CHEMBL3929592 1 5.00
CHEMBL3934622 1 4.94
CHEMBL3982251 1 4.93
CHEMBL3954284 1 4.76
CHEMBL3968057 1 4.68
CHEMBL3913209 2 4.65
CHEMBL314145 1 4.16
CHEMBL3979818 1 -
CHEMBL3922756 1 -
CHEMBL3941076 1 -
CHEMBL3940595 1 -
CHEMBL3895280 1 -
CHEMBL3929308 1 -
CHEMBL3947560 1 -
CHEMBL3897460 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3906398 Ki = 410.0 nM 6.39
CHEMBL3926920 Ki = 860.0 nM 6.07
CHEMBL3915933 Ki = 1720.0 nM 5.76
CHEMBL3911902 Ki = 3240.0 nM 5.49
CHEMBL3980061 Ki = 6620.0 nM 5.18
CHEMBL3921638 Ki = 9310.0 nM 5.03
CHEMBL3929592 Ki = 9950.0 nM 5.00
CHEMBL3934622 Ki = 11590.0 nM 4.94
CHEMBL3982251 Ki = 11870.0 nM 4.93
CHEMBL3954284 Ki = 17500.0 nM 4.76
CHEMBL3968057 Ki = 20650.0 nM 4.68
CHEMBL3913209 Ki = 22370.0 nM 4.65
CHEMBL3913209 Ki = 63240.0 nM 4.20
CHEMBL314145 Ki = 69000.0 nM 4.16
CHEMBL3979818 Ki > 1000000.0 nM -
CHEMBL3922756 Ki > 1000000.0 nM -
CHEMBL3941076 Ki > 1000000.0 nM -
CHEMBL3940595 Ki > 1000000.0 nM -
CHEMBL3895280 Ki > 1000000.0 nM -
CHEMBL3929308 Ki = 500000.0 nM -
CHEMBL3947560 Ki = 356000.0 nM -
CHEMBL3897460 Ki = 232000.0 nM -