Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL902302

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

Binding
Inhibition of PKCtheta by FP assay
ChEMBL ↗
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of potent and selective PKC-theta inhibitors.
Cywin CL, Dahmann G, Prokopowicz AS, Young ER, Magolda RL, Cardozo MG, Cogan DA, Disalvo D, Ginn JD, Kashem MA, Wolak JP, Homon CA, Farrell TM, Grbic H, Hu H, Kaplita PV, Liu LH, Spero DM, Jeanfavre DD, O'Shea KM, White DM, Woska JR, Brown ML.
Bioorg Med Chem Lett (2007) 17 : 225 -230
PubMed 17055721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 7.00 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL246365 — — 1 8.52
CHEMBL392642 — — 1 8.30
CHEMBL246175 — — 1 8.30
CHEMBL246174 — — 1 8.22
CHEMBL246386 — — 1 8.15
CHEMBL246183 — — 1 8.10
CHEMBL396929 — — 1 7.96
CHEMBL247979 — — 1 7.92
CHEMBL245912 — — 1 7.89
CHEMBL245977 — — 1 7.82
CHEMBL395690 — — 1 7.77
CHEMBL246159 — — 1 7.75
CHEMBL248183 — — 1 7.75
CHEMBL245783 — — 1 7.66
CHEMBL246184 — — 1 7.57
CHEMBL395691 — — 1 7.54
CHEMBL247572 — — 1 7.51
CHEMBL428751 — — 1 7.47
CHEMBL396370 — — 1 7.46
CHEMBL246177 — — 1 7.41
CHEMBL438669 — — 1 7.41
CHEMBL246182 — — 1 7.38
CHEMBL246387 — — 1 7.34
CHEMBL246970 — — 1 7.34
CHEMBL395689 — — 1 7.32
CHEMBL391610 — — 1 7.27
CHEMBL246160 — — 1 7.27
CHEMBL396924 — — 1 7.22
CHEMBL247377 — — 1 7.11
CHEMBL245757 — — 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL246365 — IC50 = 3.0 nM 8.52
CHEMBL392642 — IC50 = 5.0 nM 8.30
CHEMBL246175 — IC50 = 5.0 nM 8.30
CHEMBL246174 — IC50 = 6.0 nM 8.22
CHEMBL246386 — IC50 = 7.0 nM 8.15
CHEMBL246183 — IC50 = 8.0 nM 8.10
CHEMBL396929 — IC50 = 11.0 nM 7.96
CHEMBL247979 — IC50 = 12.0 nM 7.92
CHEMBL245912 — IC50 = 13.0 nM 7.89
CHEMBL245977 — IC50 = 15.0 nM 7.82
CHEMBL395690 — IC50 = 17.0 nM 7.77
CHEMBL246159 — IC50 = 18.0 nM 7.75
CHEMBL248183 — IC50 = 18.0 nM 7.75
CHEMBL245783 — IC50 = 22.0 nM 7.66
CHEMBL246184 — IC50 = 27.0 nM 7.57
CHEMBL395691 — IC50 = 29.0 nM 7.54
CHEMBL247572 — IC50 = 31.0 nM 7.51
CHEMBL428751 — IC50 = 34.0 nM 7.47
CHEMBL396370 — IC50 = 35.0 nM 7.46
CHEMBL246177 — IC50 = 39.0 nM 7.41
CHEMBL438669 — IC50 = 39.0 nM 7.41
CHEMBL246182 — IC50 = 42.0 nM 7.38
CHEMBL246387 — IC50 = 46.0 nM 7.34
CHEMBL246970 — IC50 = 46.0 nM 7.34
CHEMBL395689 — IC50 = 48.0 nM 7.32
CHEMBL391610 — IC50 = 54.0 nM 7.27
CHEMBL246160 — IC50 = 54.0 nM 7.27
CHEMBL396924 — IC50 = 60.0 nM 7.22
CHEMBL247377 — IC50 = 77.0 nM 7.11
CHEMBL245757 — IC50 = 83.0 nM 7.08
CHEMBL437941 — IC50 = 85.0 nM 7.07
CHEMBL391609 — IC50 = 90.0 nM 7.05
CHEMBL246161 — IC50 = 90.0 nM 7.05
CHEMBL247573 — IC50 = 94.0 nM 7.03
CHEMBL245982 — IC50 = 100.0 nM 7.00
CHEMBL246367 — IC50 = 110.0 nM 6.96
CHEMBL247177 — IC50 = 130.0 nM 6.89
CHEMBL391753 — IC50 = 160.0 nM 6.80
CHEMBL246972 — IC50 = 170.0 nM 6.77
CHEMBL247176 — IC50 = 180.0 nM 6.75
CHEMBL391754 — IC50 = 200.0 nM 6.70
CHEMBL395160 — IC50 = 210.0 nM 6.68
CHEMBL245958 — IC50 = 210.0 nM 6.68
CHEMBL397397 — IC50 = 270.0 nM 6.57
CHEMBL394113 — IC50 = 400.0 nM 6.40
CHEMBL246366 — IC50 = 450.0 nM 6.35
CHEMBL246550 — IC50 = 460.0 nM 6.34
CHEMBL247571 — IC50 = 500.0 nM 6.30
CHEMBL247376 — IC50 = 640.0 nM 6.19
CHEMBL394069 — IC50 = 680.0 nM 6.17