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Assay Detail

CHEMBL5738331

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

Binding
MAPK13 and MAPK14 enzyme assays: ach of these analogs were checked for physical chemical characteristics based on molecular weight, Lipinski's Rule of 5, partition coefficient (log P), and topological polar surface area (tPSA). Acceptable analogs were assessed for IC50 in MAPK13 and MAPK14 enzyme assays, using inhibition of the closely related MAPK14 as a surrogate for specificity against the broader kinome.
ChEMBL ↗
375
Total Activities
118
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 14 (CHEMBL260) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mitogen-activated protein kinase inhibitors, methods of making, and methods of use thereof
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 125 6.74 8.40
kon 125 - -
k_off 125 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5935130 — — 6 8.40
CHEMBL5792316 — — 3 8.30
CHEMBL5760386 — — 6 8.30
CHEMBL103667 DORAMAPIMOD 2.0 3 8.30
CHEMBL5830188 — — 3 8.22
CHEMBL5772598 — — 6 8.22
CHEMBL5973731 — — 3 8.15
CHEMBL6005903 — — 3 8.15
CHEMBL5815047 — — 3 8.15
CHEMBL5994239 — — 3 8.15
CHEMBL5788002 — — 3 7.96
CHEMBL5852736 — — 3 7.96
CHEMBL5868979 — — 3 7.92
CHEMBL5860468 — — 3 7.82
CHEMBL6017241 — — 3 7.77
CHEMBL5999321 — — 3 7.75
CHEMBL5759964 — — 3 7.72
CHEMBL5806948 — — 3 7.68
CHEMBL5865108 — — 3 7.64
CHEMBL5913459 — — 3 7.62
CHEMBL5870140 — — 3 7.55
CHEMBL5965421 — — 3 7.51
CHEMBL5995808 — — 3 7.44
CHEMBL5987807 — — 3 7.43
CHEMBL5932225 — — 3 7.43
CHEMBL5942158 — — 3 7.40
CHEMBL6004961 — — 3 7.40
CHEMBL6042780 — — 3 7.29
CHEMBL6014440 — — 3 7.28
CHEMBL5748471 — — 3 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5935130 — IC50 = 4.0 nM 8.40
CHEMBL5935130 — IC50 = 4.0 nM 8.40
CHEMBL103667 DORAMAPIMOD IC50 = 5.0 nM 8.30
CHEMBL5792316 — IC50 = 5.0 nM 8.30
CHEMBL5760386 — IC50 = 5.0 nM 8.30
CHEMBL5760386 — IC50 = 5.0 nM 8.30
CHEMBL5772598 — IC50 = 6.0 nM 8.22
CHEMBL5830188 — IC50 = 6.0 nM 8.22
CHEMBL5772598 — IC50 = 6.0 nM 8.22
CHEMBL6005903 — IC50 = 7.0 nM 8.15
CHEMBL5973731 — IC50 = 7.0 nM 8.15
CHEMBL5815047 — IC50 = 7.0 nM 8.15
CHEMBL5994239 — IC50 = 7.0 nM 8.15
CHEMBL5788002 — IC50 = 11.0 nM 7.96
CHEMBL5852736 — IC50 = 11.0 nM 7.96
CHEMBL5868979 — IC50 = 12.0 nM 7.92
CHEMBL5860468 — IC50 = 15.0 nM 7.82
CHEMBL6017241 — IC50 = 17.0 nM 7.77
CHEMBL5999321 — IC50 = 18.0 nM 7.75
CHEMBL5759964 — IC50 = 19.0 nM 7.72
CHEMBL5806948 — IC50 = 21.0 nM 7.68
CHEMBL5865108 — IC50 = 23.0 nM 7.64
CHEMBL5913459 — IC50 = 24.0 nM 7.62
CHEMBL5870140 — IC50 = 28.0 nM 7.55
CHEMBL5965421 — IC50 = 31.0 nM 7.51
CHEMBL5995808 — IC50 = 36.0 nM 7.44
CHEMBL5987807 — IC50 = 37.0 nM 7.43
CHEMBL5932225 — IC50 = 37.0 nM 7.43
CHEMBL6004961 — IC50 = 40.0 nM 7.40
CHEMBL5942158 — IC50 = 40.0 nM 7.40
CHEMBL6042780 — IC50 = 51.0 nM 7.29
CHEMBL6014440 — IC50 = 52.0 nM 7.28
CHEMBL5748471 — IC50 = 62.0 nM 7.21
CHEMBL6042854 — IC50 = 64.0 nM 7.19
CHEMBL5752939 — IC50 = 67.0 nM 7.17
CHEMBL6029778 — IC50 = 67.0 nM 7.17
CHEMBL5833460 — IC50 = 83.0 nM 7.08
CHEMBL5833248 — IC50 = 90.0 nM 7.05
CHEMBL5914007 — IC50 = 94.0 nM 7.03
CHEMBL5790944 — IC50 = 95.0 nM 7.02
CHEMBL5881559 — IC50 = 114.0 nM 6.94
CHEMBL5749698 — IC50 = 122.0 nM 6.91
CHEMBL5830725 — IC50 = 129.0 nM 6.89
CHEMBL5830725 — IC50 = 129.0 nM 6.89
CHEMBL5743603 — IC50 = 139.0 nM 6.86
CHEMBL5743603 — IC50 = 139.0 nM 6.86
CHEMBL5918166 — IC50 = 148.0 nM 6.83
CHEMBL5773500 — IC50 = 171.0 nM 6.77
CHEMBL5922520 — IC50 = 181.0 nM 6.74
CHEMBL5915885 — IC50 = 193.0 nM 6.71