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Assay Detail

CHEMBL4019404

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Binding
Inhibition of P38 alpha MAPK in human whole blood assessed as reduction in TNF-alpha release after 10 mins by ELISA
ChEMBL ↗
70
Total Activities
70
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

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

Publication

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.
Walter NM, Wentsch HK, Bührmann M, Bauer SM, Döring E, Mayer-Wrangowski S, Sievers-Engler A, Willemsen-Seegers N, Zaman G, Buijsman R, Lämmerhofer M, Rauh D, Laufer SA.
J Med Chem (2017) 60 : 8027 -8054
PubMed 28834431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 70 7.05 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4074237 — — 1 9.55
CHEMBL4061369 — — 1 7.60
CHEMBL4093914 — — 1 7.51
CHEMBL4071095 — — 1 7.50
CHEMBL4103539 — — 1 7.46
CHEMBL4092372 — — 1 7.46
CHEMBL4078249 — — 1 7.45
CHEMBL4077602 — — 1 7.44
CHEMBL2316207 FS-694 — 1 7.42
CHEMBL4087408 — — 1 7.38
CHEMBL4061315 — — 1 7.37
CHEMBL4079527 — — 1 7.37
CHEMBL4088396 — — 1 7.33
CHEMBL4066023 — — 1 7.23
CHEMBL4066347 — — 1 7.22
CHEMBL4102537 — — 1 7.16
CHEMBL4103781 — — 1 7.16
CHEMBL4066269 — — 1 7.09
CHEMBL4101643 — — 1 7.04
CHEMBL4076170 — — 1 7.03
CHEMBL4082939 — — 1 7.02
CHEMBL4071599 — — 1 6.97
CHEMBL4103149 — — 1 6.86
CHEMBL4076950 — — 1 6.82
CHEMBL4103486 — — 1 6.79
CHEMBL4082844 — — 1 6.77
CHEMBL4083921 — — 1 6.74
CHEMBL4069033 — — 1 6.72
CHEMBL4065681 — — 1 6.71
CHEMBL4066610 — — 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4074237 — IC50 = 0.28 nM 9.55
CHEMBL4061369 — IC50 = 25.1 nM 7.60
CHEMBL4093914 — IC50 = 31.0 nM 7.51
CHEMBL4071095 — IC50 = 32.0 nM 7.50
CHEMBL4103539 — IC50 = 35.0 nM 7.46
CHEMBL4092372 — IC50 = 34.7 nM 7.46
CHEMBL4078249 — IC50 = 35.7 nM 7.45
CHEMBL4077602 — IC50 = 36.6 nM 7.44
CHEMBL2316207 FS-694 IC50 = 38.0 nM 7.42
CHEMBL4087408 — IC50 = 42.2 nM 7.38
CHEMBL4061315 — IC50 = 43.0 nM 7.37
CHEMBL4079527 — IC50 = 43.2 nM 7.37
CHEMBL4088396 — IC50 = 47.2 nM 7.33
CHEMBL4066023 — IC50 = 59.3 nM 7.23
CHEMBL4066347 — IC50 = 60.2 nM 7.22
CHEMBL4102537 — IC50 = 69.1 nM 7.16
CHEMBL4103781 — IC50 = 69.0 nM 7.16
CHEMBL4066269 — IC50 = 81.8 nM 7.09
CHEMBL4101643 — IC50 = 90.5 nM 7.04
CHEMBL4076170 — IC50 = 94.3 nM 7.03
CHEMBL4082939 — IC50 = 95.8 nM 7.02
CHEMBL4071599 — IC50 = 107.3 nM 6.97
CHEMBL4103149 — IC50 = 137.8 nM 6.86
CHEMBL4076950 — IC50 = 151.5 nM 6.82
CHEMBL4103486 — IC50 = 161.8 nM 6.79
CHEMBL4082844 — IC50 = 168.5 nM 6.77
CHEMBL4083921 — IC50 = 182.3 nM 6.74
CHEMBL4069033 — IC50 = 192.1 nM 6.72
CHEMBL4065681 — IC50 = 193.2 nM 6.71
CHEMBL4066610 — IC50 = 294.9 nM 6.53
CHEMBL4087104 — IC50 = 304.8 nM 6.52
CHEMBL4077106 — IC50 = 382.4 nM 6.42
CHEMBL4095093 — IC50 = 463.8 nM 6.33
CHEMBL4079228 — IC50 = 690.6 nM 6.16
CHEMBL4095732 — IC50 = 903.2 nM 6.04
CHEMBL4072511 — IC50 = 1613.6 nM 5.79
CHEMBL4068060 — IC50 - — -
CHEMBL4064695 — IC50 - — -
CHEMBL4084589 — IC50 - — -
CHEMBL4066327 — IC50 - — -
CHEMBL4059727 — IC50 - — -
CHEMBL4088016 — IC50 - — -
CHEMBL4068387 — IC50 - — -
CHEMBL4105222 — IC50 - — -
CHEMBL4103075 — IC50 - — -
CHEMBL4094105 — IC50 - — -
CHEMBL4084426 — IC50 - — -
CHEMBL4075599 — IC50 - — -
CHEMBL4061811 — IC50 - — -
CHEMBL4080980 — IC50 - — -