Details of the Target

General Information of Target

Target ID LDTP07783
Target Name Mitogen-activated protein kinase kinase kinase 15 (MAP3K15)
Gene Name MAP3K15
Gene ID 389840
Synonyms
ASK3; Mitogen-activated protein kinase kinase kinase 15; EC 2.7.11.25; Apoptosis signal-regulating kinase 3; MAPK/ERK kinase kinase 15; MEK kinase 15; MEKK 15
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MESGGGNAPAGALGAASESPQCPPPPGVEGAAGPAEPDGAAEGAAGGSGEGESGGGPRRA
LRAVYVRSESSQGGAAGGPEAGARQCLLRACEAEGAHLTSVPFGELDFGETAVLDAFYDA
DVAVVDMSDVSRQPSLFYHLGVRESFDMANNVILYHDTDADTALSLKDMVTQKNTASSGN
YYFIPYIVTPCADYFCCESDAQRRASEYMQPNWDNILGPLCMPLVDRFISLLKDIHVTSC
VYYKETLLNDIRKAREKYQGEELAKELARIKLRMDNTEVLTSDIIINLLLSYRDIQDYDA
MVKLVETLEMLPTCDLADQHNIKFHYAFALNRRNSTGDREKALQIMLQVLQSCDHPGPDM
FCLCGRIYKDIFLDSDCKDDTSRDSAIEWYRKGFELQSSLYSGINLAVLLIVAGQQFETS
LELRKIGVRLNSLLGRKGSLEKMNNYWDVGQFFSVSMLAHDVGKAVQAAERLFKLKPPVW
YLRSLVQNLLLIRRFKKTIIEHSPRQERLNFWLDIIFEATNEVTNGLRFPVLVIEPTKVY
QPSYVSINNEAEERTVSLWHVSPTEMKQMHEWNFTASSIKGISLSKFDERCCFLYVHDNS
DDFQIYFSTEEQCSRFFSLVKEMITNTAGSTVELEGETDGDTLEYEYDHDANGERVVLGK
GTYGIVYAGRDLSNQVRIAIKEIPERDSRYSQPLHEEIALHKYLKHRNIVQYLGSVSENG
YIKIFMEQVPGGSLSALLRSKWGPMKEPTIKFYTKQILEGLKYLHENQIVHRDIKGDNVL
VNTYSGVVKISDFGTSKRLAGVNPCTETFTGTLQYMAPEIIDQGPRGYGAPADIWSLGCT
IIEMATSKPPFHELGEPQAAMFKVGMFKIHPEIPEALSAEARAFILSCFEPDPHKRATTA
ELLREGFLRQVNKGKKNRIAFKPSEGPRGVVLALPTQGEPMATSSSEHGSVSPDSDAQPD
ALFERTRAPRHHLGHLLSVPDESSALEDRGLASSPEDRDQGLFLLRKDSERRAILYKILW
EEQNQVASNLQECVAQSSEELHLSVGHIKQIIGILRDFIRSPEHRVMATTISKLKVDLDF
DSSSISQIHLVLFGFQDAVNKILRNHLIRPHWMFAMDNIIRRAVQAAVTILIPELRAHFE
PTCETEGVDKDMDEAEEGYPPATGPGQEAQPHQQHLSLQLGELRQETNRLLEHLVEKERE
YQNLLRQTLEQKTQELYHLQLKLKSNCITENPAGPYGQRTDKELIDWLRLQGADAKTIEK
IVEEGYTLSDILNEITKEDLRYLRLRGGLLCRLWSAVSQYRRAQEASETKDKA
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase kinase subfamily
Function
Serine/threonine kinase which acts as a component of the MAP kinase signal transduction pathway. Once activated, acts as an upstream activator of the p38 MAPK signal transduction cascade through the phosphorylation and activation of several MAP kinase kinases. May function in a signal transduction pathway that is activated by various cell stresses and leads to apoptosis. Involved in phosphorylation of WNK4 in response to osmotic stress or hypotonic low-chloride stimulation via the p38 MAPK signal transduction cascade.
Uniprot ID
Q6ZN16
Ensemble ID
ENST00000338883.9
HGNC ID
HGNC:31689
ChEMBL ID
CHEMBL1163127

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.H765Y .
ICC12 SNV: p.A12T .
KASUMI2 SNV: p.Y721H .
KMS12BM SNV: p.E395Q .
KYSE30 SNV: p.E611D .
MCC26 SNV: p.E1186K .
MEWO SNV: p.E306K; p.W572Ter .
MFE319 SNV: p.Y208H .
MOLT4 SNV: p.P223H .
NCIH1944 Insertion: p.L409FfsTer10 .
OCILY3 SNV: p.D121Y .
RL952 SNV: p.P24S; p.R918Ter .
SW1271 SNV: p.A628V .
TOV21G SNV: p.G104W .
WM115 SNV: p.W1112Ter .
WM2664 Insertion: p.P730RfsTer33
SNV: p.W1112Ter		 .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C1143(0.73)  LDD1507  [1]
IA-alkyne
 Probe Info  		N.A.  LDD0166  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C1143(0.73)  LDD1507  [1]
 LDCM0215  AC10 HEK-293T C1143(1.07)  LDD1508  [1]
 LDCM0276  AC17 HEK-293T C1143(1.02)  LDD1515  [1]
 LDCM0277  AC18 HEK-293T C1143(1.12)  LDD1516  [1]
 LDCM0279  AC2 HEK-293T C1143(1.16)  LDD1518  [1]
 LDCM0285  AC25 HEK-293T C1143(0.87)  LDD1524  [1]
 LDCM0286  AC26 HEK-293T C1143(1.03)  LDD1525  [1]
 LDCM0294  AC33 HEK-293T C1143(0.92)  LDD1533  [1]
 LDCM0295  AC34 HEK-293T C1143(0.95)  LDD1534  [1]
 LDCM0303  AC41 HEK-293T C1143(0.73)  LDD1542  [1]
 LDCM0304  AC42 HEK-293T C1143(1.16)  LDD1543  [1]
 LDCM0311  AC49 HEK-293T C1143(0.90)  LDD1550  [1]
 LDCM0313  AC50 HEK-293T C1143(0.90)  LDD1552  [1]
 LDCM0320  AC57 HEK-293T C1143(0.91)  LDD1559  [1]
 LDCM0321  AC58 HEK-293T C1143(1.01)  LDD1560  [1]
 LDCM0356  AKOS034007680 HEK-293T C1143(0.88)  LDD1570  [1]
 LDCM0404  CL17 HEK-293T C1143(1.00)  LDD1608  [1]
 LDCM0405  CL18 HEK-293T C1143(1.09)  LDD1609  [1]
 LDCM0417  CL29 HEK-293T C1143(0.86)  LDD1621  [1]
 LDCM0419  CL30 HEK-293T C1143(0.87)  LDD1623  [1]
 LDCM0431  CL41 HEK-293T C1143(1.05)  LDD1635  [1]
 LDCM0432  CL42 HEK-293T C1143(1.16)  LDD1636  [1]
 LDCM0440  CL5 HEK-293T C1143(1.02)  LDD1644  [1]
 LDCM0444  CL53 HEK-293T C1143(0.97)  LDD1647  [1]
 LDCM0445  CL54 HEK-293T C1143(1.01)  LDD1648  [1]
 LDCM0451  CL6 HEK-293T C1143(0.95)  LDD1654  [1]
 LDCM0457  CL65 HEK-293T C1143(1.08)  LDD1660  [1]
 LDCM0458  CL66 HEK-293T C1143(1.06)  LDD1661  [1]
 LDCM0470  CL77 HEK-293T C1143(1.00)  LDD1673  [1]
 LDCM0471  CL78 HEK-293T C1143(0.89)  LDD1674  [1]
 LDCM0483  CL89 HEK-293T C1143(0.83)  LDD1686  [1]
 LDCM0485  CL90 HEK-293T C1143(0.93)  LDD1688  [1]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010

References

1 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402
2 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060