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Assay Detail

CHEMBL1061091

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Binding
Binding constant for full-length p38-alpha
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A quantitative analysis of kinase inhibitor selectivity.
Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT, Faraoni R, Floyd M, Hunt JP, Lockhart DJ, Milanov ZV, Morrison MJ, Pallares G, Patel HK, Pritchard S, Wodicka LM, Zarrinkar PP.
Nat Biotechnol (2008) 26 : 127 -132
PubMed 18183025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 38 7.86 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103667 DORAMAPIMOD 2.0 1 9.43
CHEMBL119385 NEFLAMAPIMOD 2.0 1 8.55
CHEMBL278041 SB-202190 1 8.01
CHEMBL10 SB-203580 1 7.92
CHEMBL5416410 DASATINIB 4.0 1 7.57
CHEMBL574738 AST-487 1.0 1 7.14
CHEMBL1336 SORAFENIB 4.0 1 6.43
CHEMBL572878 TOZASERTIB 2.0 1 -
CHEMBL483321 CP-724714 2.0 1 -
CHEMBL24828 VANDETANIB 4.0 1 -
CHEMBL607707 PELITINIB 2.0 1 -
CHEMBL572881 MOTESANIB 3.0 1 -
CHEMBL215152 DEFOSBARASERTIB 2.0 1 -
CHEMBL296468 BMS-387032 1.0 1 -
CHEMBL522892 DOVITINIB 3.0 1 -
CHEMBL558752 RAF-265 2.0 1 -
CHEMBL31965 CANERTINIB 3.0 1 -
CHEMBL221959 TOFACITINIB 4.0 1 -
CHEMBL535 SUNITINIB 4.0 1 -
CHEMBL1721885 SU-014813 2.0 1 -
CHEMBL388978 STAUROSPORINE 1 -
CHEMBL191003 JNJ-7706621 1 -
CHEMBL14762 SELICICLIB 2.0 1 -
CHEMBL101253 VATALANIB 3.0 1 -
CHEMBL608533 MIDOSTAURIN 4.0 1 -
CHEMBL573339 PI-103 1 -
CHEMBL259084 MLN-8054 1.0 1 -
CHEMBL124660 TANDUTINIB 2.0 1 -
CHEMBL91829 RUBOXISTAURIN 3.0 1 -
CHEMBL440084 SB-431542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103667 DORAMAPIMOD Kd = 0.37 nM 9.43
CHEMBL119385 NEFLAMAPIMOD Kd = 2.8 nM 8.55
CHEMBL278041 SB-202190 Kd = 9.8 nM 8.01
CHEMBL10 SB-203580 Kd = 12.0 nM 7.92
CHEMBL5416410 DASATINIB Kd = 27.0 nM 7.57
CHEMBL574738 AST-487 Kd = 73.0 nM 7.14
CHEMBL1336 SORAFENIB Kd = 370.0 nM 6.43
CHEMBL215152 DEFOSBARASERTIB Kd > 10000.0 nM -
CHEMBL223360 LINIFANIB Kd > 10000.0 nM -
CHEMBL296468 BMS-387032 Kd > 10000.0 nM -
CHEMBL522892 DOVITINIB Kd > 10000.0 nM -
CHEMBL558752 RAF-265 Kd > 10000.0 nM -
CHEMBL31965 CANERTINIB Kd > 10000.0 nM -
CHEMBL221959 TOFACITINIB Kd > 10000.0 nM -
CHEMBL483321 CP-724714 Kd > 10000.0 nM -
CHEMBL554 LAPATINIB Kd > 10000.0 nM -
CHEMBL553 ERLOTINIB Kd > 10000.0 nM -
CHEMBL428690 ALVOCIDIB Kd > 10000.0 nM -
CHEMBL939 GEFITINIB Kd > 10000.0 nM -
CHEMBL261849 GW632580X Kd > 10000.0 nM -
CHEMBL477772 PAZOPANIB Kd > 10000.0 nM -
CHEMBL941 IMATINIB Kd > 10000.0 nM -
CHEMBL572881 MOTESANIB Kd > 10000.0 nM -
CHEMBL607707 PELITINIB Kd > 10000.0 nM -
CHEMBL24828 VANDETANIB Kd > 10000.0 nM -
CHEMBL572878 TOZASERTIB Kd > 10000.0 nM -
CHEMBL535 SUNITINIB Kd > 10000.0 nM -
CHEMBL1721885 SU-014813 Kd > 10000.0 nM -
CHEMBL388978 STAUROSPORINE Kd > 10000.0 nM -
CHEMBL191003 JNJ-7706621 Kd > 10000.0 nM -
CHEMBL14762 SELICICLIB Kd > 10000.0 nM -
CHEMBL101253 VATALANIB Kd > 10000.0 nM -
CHEMBL608533 MIDOSTAURIN Kd > 10000.0 nM -
CHEMBL573339 PI-103 Kd > 10000.0 nM -
CHEMBL259084 MLN-8054 Kd > 10000.0 nM -
CHEMBL124660 TANDUTINIB Kd > 10000.0 nM -
CHEMBL91829 RUBOXISTAURIN Kd > 10000.0 nM -
CHEMBL440084 SB-431542 Kd > 10000.0 nM -