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Assay Detail

CHEMBL5040129

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

Binding
Binding affinity to human PIP5K2C (M1/A421) WT expressed in mammalian system assessed as dissociation constant measured at 1 uM by DiscoveRx KINOMEscan assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and Synthesis of Pyrrolo[2,3-<i>d</i>]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate.
Williamson DS, Smith GP, Mikkelsen GK, Jensen T, Acheson-Dossang P, Badolo L, Bedford ST, Chell V, Chen IJ, Dokurno P, Hentzer M, Newland S, Ray SC, Shaw T, Surgenor AE, Terry L, Wang Y, Christensen KV.
J Med Chem (2021) 64 : 10312 -10332
PubMed 34184879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 6.55 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087055 1 6.72
CHEMBL5092087 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087055 Kd = 190.0 nM 6.72
CHEMBL5092087 Kd = 430.0 nM 6.37