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Assay Detail

CHEMBL1936697

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

Binding
Inhibition of human RSK2
22
Total Activities
22
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

Ribosomal protein S6 kinase alpha-3 (CHEMBL2345)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.
Kirrane TM, Boyer SJ, Burke J, Guo X, Snow RJ, Soleymanzadeh L, Swinamer A, Zhang Y, Madwed JB, Kashem M, Kugler S, O'Neill MM.
Bioorg Med Chem Lett (2012) 22 : 738 -742
PubMed 22056746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.96 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1933280 1 9.00
CHEMBL1933288 1 9.00
CHEMBL1933278 1 8.70
CHEMBL1933287 1 8.40
CHEMBL1933284 1 8.22
CHEMBL1933149 1 8.15
CHEMBL1933279 1 8.05
CHEMBL1933277 1 8.00
CHEMBL1933148 1 7.96
CHEMBL1933285 1 7.92
CHEMBL1933147 1 7.89
CHEMBL1933289 1 7.85
CHEMBL1933068 1 7.75
CHEMBL1933143 1 7.72
CHEMBL1933281 1 7.70
CHEMBL1933286 1 7.70
CHEMBL1933283 1 7.68
CHEMBL1933145 1 7.58
CHEMBL1933290 1 7.57
CHEMBL1933282 1 7.21
CHEMBL1933146 1 7.07
CHEMBL1933144 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1933280 IC50 = 1.0 nM 9.00
CHEMBL1933288 IC50 = 1.0 nM 9.00
CHEMBL1933278 IC50 = 2.0 nM 8.70
CHEMBL1933287 IC50 = 4.0 nM 8.40
CHEMBL1933284 IC50 = 6.0 nM 8.22
CHEMBL1933149 IC50 = 7.0 nM 8.15
CHEMBL1933279 IC50 = 9.0 nM 8.05
CHEMBL1933277 IC50 = 10.0 nM 8.00
CHEMBL1933148 IC50 = 11.0 nM 7.96
CHEMBL1933285 IC50 = 12.0 nM 7.92
CHEMBL1933147 IC50 = 13.0 nM 7.89
CHEMBL1933289 IC50 = 14.0 nM 7.85
CHEMBL1933068 IC50 = 18.0 nM 7.75
CHEMBL1933143 IC50 = 19.0 nM 7.72
CHEMBL1933281 IC50 = 20.0 nM 7.70
CHEMBL1933286 IC50 = 20.0 nM 7.70
CHEMBL1933283 IC50 = 21.0 nM 7.68
CHEMBL1933145 IC50 = 26.0 nM 7.58
CHEMBL1933290 IC50 = 27.0 nM 7.57
CHEMBL1933282 IC50 = 61.0 nM 7.21
CHEMBL1933146 IC50 = 86.0 nM 7.07
CHEMBL1933144 IC50 > 10000.0 nM -