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Assay Detail

CHEMBL1648826

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

Binding
Inhibition of recombinant JNK2 after 60 mins by TR-FRET assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I.
Bioorg Med Chem Lett (2011) 21 : 315 -319
PubMed 21112785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.43 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1644646 1 7.24
CHEMBL1644638 1 7.21
CHEMBL1644618 1 7.16
CHEMBL1644615 1 7.03
CHEMBL1644639 1 7.01
CHEMBL1644642 1 7.01
CHEMBL1644625 1 6.96
CHEMBL1644619 1 6.89
CHEMBL1644641 1 6.82
CHEMBL1644637 1 6.82
CHEMBL1644645 1 6.77
CHEMBL1644632 1 6.72
CHEMBL1644622 1 6.66
CHEMBL1644620 1 6.60
CHEMBL1644640 1 6.50
CHEMBL1644621 1 6.46
CHEMBL1644635 1 6.42
CHEMBL1644623 1 6.41
CHEMBL1644630 1 6.36
CHEMBL1644624 1 6.33
CHEMBL1644643 1 6.28
CHEMBL1644636 1 6.24
CHEMBL1644627 1 6.19
CHEMBL1644634 1 6.11
CHEMBL1644626 1 6.02
CHEMBL1644629 1 5.82
CHEMBL1644644 1 5.70
CHEMBL1644631 1 5.36
CHEMBL1644633 1 5.28
CHEMBL1644617 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1644646 IC50 = 58.0 nM 7.24
CHEMBL1644638 IC50 = 61.0 nM 7.21
CHEMBL1644618 IC50 = 69.0 nM 7.16
CHEMBL1644615 IC50 = 93.0 nM 7.03
CHEMBL1644639 IC50 = 97.0 nM 7.01
CHEMBL1644642 IC50 = 97.0 nM 7.01
CHEMBL1644625 IC50 = 110.0 nM 6.96
CHEMBL1644619 IC50 = 130.0 nM 6.89
CHEMBL1644641 IC50 = 150.0 nM 6.82
CHEMBL1644637 IC50 = 150.0 nM 6.82
CHEMBL1644645 IC50 = 170.0 nM 6.77
CHEMBL1644632 IC50 = 190.0 nM 6.72
CHEMBL1644622 IC50 = 220.0 nM 6.66
CHEMBL1644620 IC50 = 250.0 nM 6.60
CHEMBL1644640 IC50 = 320.0 nM 6.50
CHEMBL1644621 IC50 = 350.0 nM 6.46
CHEMBL1644635 IC50 = 380.0 nM 6.42
CHEMBL1644623 IC50 = 390.0 nM 6.41
CHEMBL1644630 IC50 = 440.0 nM 6.36
CHEMBL1644624 IC50 = 470.0 nM 6.33
CHEMBL1644643 IC50 = 530.0 nM 6.28
CHEMBL1644636 IC50 = 570.0 nM 6.24
CHEMBL1644627 IC50 = 650.0 nM 6.19
CHEMBL1644634 IC50 = 780.0 nM 6.11
CHEMBL1644626 IC50 = 950.0 nM 6.02
CHEMBL1644629 IC50 = 1500.0 nM 5.82
CHEMBL1644644 IC50 = 2000.0 nM 5.70
CHEMBL1644631 IC50 = 4400.0 nM 5.36
CHEMBL1644633 IC50 = 5300.0 nM 5.28
CHEMBL1644617 IC50 = 32000.0 nM 4.50
CHEMBL1644628 IC50 > 5000.0 nM -