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Assay Detail

CHEMBL3265733

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

Binding
Binding affinity to human acrylodan-labeled N-terminal His-tagged DDR2 (558 to 855 aa) by FLiK assay
32
Total Activities
32
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

Discoidin domain-containing receptor 2 (CHEMBL5122)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of type II and III DDR2 inhibitors.
Richters A, Nguyen HD, Phan T, Simard JR, Grütter C, Engel J, Rauh D.
J Med Chem (2014) 57 : 4252 -4262
PubMed 24754677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 32 6.85 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL568875 1 7.82
CHEMBL498947 1 7.82
CHEMBL5416410 DASATINIB 4.0 1 7.75
CHEMBL344800 1 7.70
CHEMBL103667 DORAMAPIMOD 2.0 1 7.68
CHEMBL3261118 1 7.52
CHEMBL1738943 1 7.20
CHEMBL255863 NILOTINIB 4.0 1 7.12
CHEMBL2403816 1 7.03
CHEMBL522387 1 6.75
CHEMBL420047 1 6.60
CHEMBL1336 SORAFENIB 4.0 1 6.50
CHEMBL1738945 1 6.42
CHEMBL1940504 1 6.42
CHEMBL1940500 1 6.39
CHEMBL583263 1 6.38
CHEMBL253969 OSI-632 2.0 1 6.38
CHEMBL3261116 1 6.37
CHEMBL578172 1 6.37
CHEMBL477772 PAZOPANIB 4.0 1 6.24
CHEMBL1738946 1 6.15
CHEMBL3261119 1 6.04
CHEMBL3261120 1 -
CHEMBL87580 1 -
CHEMBL572878 TOZASERTIB 2.0 1 -
CHEMBL3261121 1 -
CHEMBL476011 1 -
CHEMBL1738942 1 -
CHEMBL2403875 1 -
CHEMBL3261117 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL568875 Kd = 15.0 nM 7.82
CHEMBL498947 Kd = 15.0 nM 7.82
CHEMBL5416410 DASATINIB Kd = 18.0 nM 7.75
CHEMBL344800 Kd = 20.0 nM 7.70
CHEMBL103667 DORAMAPIMOD Kd = 21.0 nM 7.68
CHEMBL3261118 Kd = 30.0 nM 7.52
CHEMBL1738943 Kd = 63.0 nM 7.20
CHEMBL255863 NILOTINIB Kd = 75.0 nM 7.12
CHEMBL2403816 Kd = 93.0 nM 7.03
CHEMBL522387 Kd = 178.0 nM 6.75
CHEMBL420047 Kd = 252.0 nM 6.60
CHEMBL1336 SORAFENIB Kd = 313.0 nM 6.50
CHEMBL1738945 Kd = 382.0 nM 6.42
CHEMBL1940504 Kd = 385.0 nM 6.42
CHEMBL1940500 Kd = 406.0 nM 6.39
CHEMBL253969 OSI-632 Kd = 422.0 nM 6.38
CHEMBL583263 Kd = 412.0 nM 6.38
CHEMBL3261116 Kd = 424.0 nM 6.37
CHEMBL578172 Kd = 428.0 nM 6.37
CHEMBL477772 PAZOPANIB Kd = 581.0 nM 6.24
CHEMBL1738946 Kd = 702.0 nM 6.15
CHEMBL3261119 Kd = 915.0 nM 6.04
CHEMBL3261120 Kd > 1000.0 nM -
CHEMBL87580 Kd > 1000.0 nM -
CHEMBL572878 TOZASERTIB Kd > 2500.0 nM -
CHEMBL3261121 Kd > 1000.0 nM -
CHEMBL476011 Kd > 1000.0 nM -
CHEMBL1738942 Kd > 1000.0 nM -
CHEMBL2403875 Kd > 1000.0 nM -
CHEMBL3261117 Kd > 1000.0 nM -
CHEMBL1940505 Kd > 1000.0 nM -
CHEMBL1940503 Kd > 1000.0 nM -