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Assay Detail

CHEMBL5734103

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

Binding
Inhibition Assay: The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP.
ChEMBL ↗
252
Total Activities
80
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Leucyl-cystinyl aminopeptidase (CHEMBL3712) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyridine derivatives
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 84 7.82 9.24
kon 84 - -
k_off 84 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5903806 — — 3 9.24
CHEMBL5911053 — — 3 9.19
CHEMBL6060186 — — 3 9.03
CHEMBL6063038 — — 3 8.92
CHEMBL6024927 — — 3 8.85
CHEMBL5932762 — — 3 8.82
CHEMBL5791361 — — 3 8.82
CHEMBL5803943 — — 3 8.80
CHEMBL5848513 — — 3 8.77
CHEMBL5795417 — — 3 8.77
CHEMBL5958561 — — 6 8.74
CHEMBL5808534 — — 3 8.74
CHEMBL5832794 — — 3 8.64
CHEMBL5920216 — — 3 8.62
CHEMBL6051200 — — 3 8.60
CHEMBL5810387 — — 3 8.57
CHEMBL5786989 — — 3 8.55
CHEMBL6031498 — — 3 8.49
CHEMBL5776390 — — 3 8.42
CHEMBL5782578 — — 3 8.42
CHEMBL5878941 — — 3 8.36
CHEMBL5973905 — — 3 8.35
CHEMBL5804941 — — 3 8.34
CHEMBL5929919 — — 3 8.31
CHEMBL5893968 — — 3 8.29
CHEMBL5942015 — — 3 8.28
CHEMBL5904990 — — 3 8.24
CHEMBL5856899 — — 3 8.23
CHEMBL5825769 — — 3 8.23
CHEMBL5851017 — — 3 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5903806 — IC50 = 0.58 nM 9.24
CHEMBL5911053 — IC50 = 0.65 nM 9.19
CHEMBL6060186 — IC50 = 0.94 nM 9.03
CHEMBL6063038 — IC50 = 1.2 nM 8.92
CHEMBL6024927 — IC50 = 1.4 nM 8.85
CHEMBL5932762 — IC50 = 1.5 nM 8.82
CHEMBL5791361 — IC50 = 1.5 nM 8.82
CHEMBL5803943 — IC50 = 1.6 nM 8.80
CHEMBL5848513 — IC50 = 1.7 nM 8.77
CHEMBL5795417 — IC50 = 1.7 nM 8.77
CHEMBL5958561 — IC50 = 1.8 nM 8.74
CHEMBL5808534 — IC50 = 1.8 nM 8.74
CHEMBL5832794 — IC50 = 2.3 nM 8.64
CHEMBL5920216 — IC50 = 2.4 nM 8.62
CHEMBL6051200 — IC50 = 2.5 nM 8.60
CHEMBL5810387 — IC50 = 2.7 nM 8.57
CHEMBL5786989 — IC50 = 2.8 nM 8.55
CHEMBL6031498 — IC50 = 3.2 nM 8.49
CHEMBL5776390 — IC50 = 3.8 nM 8.42
CHEMBL5782578 — IC50 = 3.8 nM 8.42
CHEMBL5878941 — IC50 = 4.4 nM 8.36
CHEMBL5973905 — IC50 = 4.5 nM 8.35
CHEMBL5804941 — IC50 = 4.6 nM 8.34
CHEMBL5929919 — IC50 = 4.9 nM 8.31
CHEMBL5893968 — IC50 = 5.1 nM 8.29
CHEMBL5942015 — IC50 = 5.2 nM 8.28
CHEMBL5904990 — IC50 = 5.8 nM 8.24
CHEMBL5856899 — IC50 = 5.9 nM 8.23
CHEMBL5825769 — IC50 = 5.9 nM 8.23
CHEMBL5851017 — IC50 = 6.4 nM 8.19
CHEMBL5795510 — IC50 = 7.1 nM 8.15
CHEMBL5741750 — IC50 = 7.6 nM 8.12
CHEMBL5968090 — IC50 = 8.3 nM 8.08
CHEMBL5882544 — IC50 = 8.6 nM 8.07
CHEMBL5898578 — IC50 = 8.7 nM 8.06
CHEMBL6061316 — IC50 = 11.0 nM 7.96
CHEMBL5990802 — IC50 = 12.0 nM 7.92
CHEMBL5977264 — IC50 = 12.0 nM 7.92
CHEMBL5882123 — IC50 = 14.0 nM 7.85
CHEMBL5958233 — IC50 = 15.0 nM 7.82
CHEMBL6051663 — IC50 = 15.0 nM 7.82
CHEMBL5842220 — IC50 = 15.0 nM 7.82
CHEMBL5759225 — IC50 = 15.0 nM 7.82
CHEMBL5950877 — IC50 = 15.0 nM 7.82
CHEMBL5794922 — IC50 = 19.0 nM 7.72
CHEMBL6048632 — IC50 = 19.0 nM 7.72
CHEMBL6047330 — IC50 = 20.0 nM 7.70
CHEMBL5833051 — IC50 = 20.0 nM 7.70
CHEMBL5784802 — IC50 = 20.0 nM 7.70
CHEMBL5973066 — IC50 = 21.0 nM 7.68