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Assay Detail

CHEMBL4827844

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

Binding
Inhibition of PKA-theta (unknown origin) using Fam-labelled S6-derived peptide incubated for 2 hrs by TR-FRET assay
ChEMBL ↗
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein kinase C theta type (CHEMBL3920) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005.
Papa P, Whitefield B, Mortensen DS, Cashion D, Huang D, Torres E, Parnes J, Sapienza J, Hansen J, Correa M, Delgado M, Harris R, Hegde S, Norris S, Bahmanyar S, Plantevin-Krenitsky V, Liu Z, Leftheris K, Kulkarni A, Bennett B, Hur EM, Ringheim G, Khambatta G, Chan H, Muir J, Blease K, Burnett K, LeBrun L, Morrison L, Celeridad M, Khattri R, Cathers BE.
J Med Chem (2021) 64 : 11886 -11903
PubMed 34355886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.06 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3982723 DAROVASERTIB 2.0 1 9.40
CHEMBL4849510 — — 1 8.89
CHEMBL4853353 — — 1 8.85
CHEMBL4854104 — — 1 8.66
CHEMBL4854326 — — 1 8.40
CHEMBL4859091 — — 1 8.40
CHEMBL4851695 — — 1 8.22
CHEMBL4861883 — — 1 8.15
CHEMBL4870774 — — 1 8.15
CHEMBL4873647 — — 1 8.10
CHEMBL4867906 — — 1 7.92
CHEMBL4856779 — — 1 7.70
CHEMBL4858914 — — 1 7.70
CHEMBL4876360 — — 1 7.57
CHEMBL4858601 — — 1 7.50
CHEMBL4851347 — — 1 7.47
CHEMBL4870192 — — 1 7.42
CHEMBL4851812 — — 1 7.30
CHEMBL4875258 — — 1 7.24
CHEMBL4873755 — — 1 7.24
CHEMBL4864053 — — 1 7.16
CHEMBL4865721 — — 1 7.05
CHEMBL4856178 — — 1 7.05
CHEMBL4872717 — — 1 7.00
CHEMBL4853493 — — 1 7.00
CHEMBL4874653 — — 1 7.00
CHEMBL4849429 — — 1 6.92
CHEMBL4855568 — — 1 6.92
CHEMBL4858037 — — 1 6.89
CHEMBL4850874 — — 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3982723 DAROVASERTIB IC50 = 0.4 nM 9.40
CHEMBL4849510 — IC50 = 1.3 nM 8.89
CHEMBL4853353 — IC50 = 1.4 nM 8.85
CHEMBL4854104 — IC50 = 2.2 nM 8.66
CHEMBL4854326 — IC50 = 4.0 nM 8.40
CHEMBL4859091 — IC50 = 4.0 nM 8.40
CHEMBL4851695 — IC50 = 6.0 nM 8.22
CHEMBL4861883 — IC50 = 7.0 nM 8.15
CHEMBL4870774 — IC50 = 7.0 nM 8.15
CHEMBL4873647 — IC50 = 8.0 nM 8.10
CHEMBL4867906 — IC50 = 12.0 nM 7.92
CHEMBL4856779 — IC50 = 20.0 nM 7.70
CHEMBL4858914 — IC50 = 20.0 nM 7.70
CHEMBL4876360 — IC50 = 27.0 nM 7.57
CHEMBL4858601 — IC50 = 32.0 nM 7.50
CHEMBL4851347 — IC50 = 34.0 nM 7.47
CHEMBL4870192 — IC50 = 38.0 nM 7.42
CHEMBL4851812 — IC50 = 50.0 nM 7.30
CHEMBL4875258 — IC50 = 58.0 nM 7.24
CHEMBL4873755 — IC50 = 58.0 nM 7.24
CHEMBL4864053 — IC50 = 70.0 nM 7.16
CHEMBL4865721 — IC50 = 90.0 nM 7.05
CHEMBL4856178 — IC50 = 90.0 nM 7.05
CHEMBL4874653 — IC50 = 100.0 nM 7.00
CHEMBL4872717 — IC50 = 100.0 nM 7.00
CHEMBL4853493 — IC50 = 100.0 nM 7.00
CHEMBL4849429 — IC50 = 120.0 nM 6.92
CHEMBL4855568 — IC50 = 120.0 nM 6.92
CHEMBL4858037 — IC50 = 130.0 nM 6.89
CHEMBL4850874 — IC50 = 140.0 nM 6.85
CHEMBL4849864 — IC50 = 140.0 nM 6.85
CHEMBL4861789 — IC50 = 140.0 nM 6.85
CHEMBL4878146 — IC50 = 150.0 nM 6.82
CHEMBL4873812 — IC50 = 170.0 nM 6.77
CHEMBL4878871 — IC50 = 200.0 nM 6.70
CHEMBL4875806 — IC50 = 300.0 nM 6.52
CHEMBL4878438 — IC50 = 300.0 nM 6.52
CHEMBL4850753 — IC50 = 330.0 nM 6.48
CHEMBL4870017 — IC50 = 350.0 nM 6.46
CHEMBL4853079 — IC50 = 400.0 nM 6.40
CHEMBL4851228 — IC50 = 450.0 nM 6.35
CHEMBL4861260 — IC50 = 500.0 nM 6.30
CHEMBL4858809 — IC50 = 700.0 nM 6.16
CHEMBL4873015 — IC50 = 800.0 nM 6.10
CHEMBL4861249 — IC50 = 900.0 nM 6.05
CHEMBL4865377 — IC50 = 900.0 nM 6.05
CHEMBL4850891 — IC50 = 1100.0 nM 5.96
CHEMBL4864450 — IC50 = 1100.0 nM 5.96
CHEMBL4850342 — IC50 = 1200.0 nM 5.92
CHEMBL4872846 — IC50 = 4000.0 nM 5.40