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Assay Detail

CHEMBL5736244

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

Binding
In Vitro Assay: Assays were done by measuring the transfer of tritium from 15(S)-[15-3H] PGE2 to glutamate (at 1 μM PGE2 substrate), or by direct fluorescence monitoring of NADH generation by 15-PGDH (done at 20 μM PGE2 substrate.
282
Total Activities
91
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

15-hydroxyprostaglandin dehydrogenase [NAD(+)] (CHEMBL1293255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Compositions and methods of modulating short-chain dehydrogenase activity
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 94 8.01 9.01
kon 94 - -
k_off 94 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072253 3 9.01
CHEMBL4060121 3 8.94
CHEMBL5794676 9 8.89
CHEMBL4091103 3 8.87
CHEMBL4097930 3 8.86
CHEMBL4070824 3 8.86
CHEMBL5763449 3 8.85
CHEMBL5902819 3 8.85
CHEMBL4071206 3 8.74
CHEMBL4076946 3 8.70
CHEMBL4087830 3 8.69
CHEMBL4090222 3 8.68
CHEMBL4092806 3 8.67
CHEMBL4059682 3 8.64
CHEMBL4087985 3 8.62
CHEMBL4061483 3 8.60
CHEMBL5947102 3 8.60
CHEMBL4073304 3 8.60
CHEMBL5867179 3 8.60
CHEMBL4092188 3 8.59
CHEMBL4065965 3 8.58
CHEMBL4072938 3 8.58
CHEMBL5908068 3 8.57
CHEMBL6009480 3 8.54
CHEMBL5868063 3 8.54
CHEMBL4076321 3 8.52
CHEMBL4099821 3 8.50
CHEMBL4074740 3 8.48
CHEMBL4070888 3 8.47
CHEMBL4093974 3 8.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072253 IC50 = 0.97 nM 9.01
CHEMBL4060121 IC50 = 1.14 nM 8.94
CHEMBL5794676 IC50 = 1.3 nM 8.89
CHEMBL4091103 IC50 = 1.34 nM 8.87
CHEMBL4097930 IC50 = 1.37 nM 8.86
CHEMBL4070824 IC50 = 1.37 nM 8.86
CHEMBL5763449 IC50 = 1.43 nM 8.85
CHEMBL5902819 IC50 = 1.41 nM 8.85
CHEMBL4071206 IC50 = 1.83 nM 8.74
CHEMBL4076946 IC50 = 1.99 nM 8.70
CHEMBL4087830 IC50 = 2.05 nM 8.69
CHEMBL4090222 IC50 = 2.09 nM 8.68
CHEMBL4092806 IC50 = 2.13 nM 8.67
CHEMBL4059682 IC50 = 2.3 nM 8.64
CHEMBL4087985 IC50 = 2.4 nM 8.62
CHEMBL5867179 IC50 = 2.5 nM 8.60
CHEMBL4073304 IC50 = 2.5 nM 8.60
CHEMBL4061483 IC50 = 2.53 nM 8.60
CHEMBL5947102 IC50 = 2.5 nM 8.60
CHEMBL5794676 IC50 = 2.6 nM 8.59
CHEMBL4092188 IC50 = 2.56 nM 8.59
CHEMBL4072938 IC50 = 2.61 nM 8.58
CHEMBL4065965 IC50 = 2.65 nM 8.58
CHEMBL5908068 IC50 = 2.71 nM 8.57
CHEMBL6009480 IC50 = 2.9 nM 8.54
CHEMBL5868063 IC50 = 2.86 nM 8.54
CHEMBL4076321 IC50 = 2.99 nM 8.52
CHEMBL4099821 IC50 = 3.16 nM 8.50
CHEMBL4074740 IC50 = 3.33 nM 8.48
CHEMBL4070888 IC50 = 3.4 nM 8.47
CHEMBL4093974 IC50 = 3.48 nM 8.46
CHEMBL4095639 IC50 = 3.45 nM 8.46
CHEMBL5844725 IC50 = 3.53 nM 8.45
CHEMBL5761918 IC50 = 3.73 nM 8.43
CHEMBL4077682 IC50 = 3.71 nM 8.43
CHEMBL5866860 IC50 = 3.99 nM 8.40
CHEMBL4082378 IC50 = 4.01 nM 8.40
CHEMBL4060870 IC50 = 3.97 nM 8.40
CHEMBL4065035 IC50 = 4.06 nM 8.39
CHEMBL5875224 IC50 = 4.18 nM 8.38
CHEMBL4064717 IC50 = 4.29 nM 8.37
CHEMBL5928952 IC50 = 4.36 nM 8.36
CHEMBL4066687 IC50 = 4.87 nM 8.31
CHEMBL4101333 IC50 = 5.27 nM 8.28
CHEMBL5840661 IC50 = 5.55 nM 8.26
CHEMBL5823316 IC50 = 5.7 nM 8.24
CHEMBL4099492 IC50 = 5.87 nM 8.23
CHEMBL4081420 IC50 = 6.14 nM 8.21
CHEMBL4074636 IC50 = 6.67 nM 8.18
CHEMBL6032546 IC50 = 7.62 nM 8.12