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Assay Detail

CHEMBL5054159

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

Binding
Inhibition of DDR2 (unknown origin) expressed in HEK293T cells using NanoBRET NanoGlo substrate incubated for 2 hrs by NanoBRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe.
Röhm S, Berger BT, Schröder M, Chatterjee D, Mathea S, Joerger AC, Pinkas DM, Bufton JC, Tjaden A, Kovooru L, Kudolo M, Pohl C, Bullock AN, Müller S, Laufer S, Knapp S.
J Med Chem (2021) 64 : 13451 -13474
PubMed 34506142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.47 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087073 1 8.30
CHEMBL4591082 SR-302 1 7.75
CHEMBL5094236 1 5.94
CHEMBL5075462 1 5.76
CHEMBL5084386 1 5.69
CHEMBL5081039 1 5.46
CHEMBL5079394 1 5.43
CHEMBL4756586 1 5.40
CHEMBL4778587 1 5.28
CHEMBL5086352 1 5.13
CHEMBL4568183 SR-301 1 4.81
CHEMBL5092076 1 4.67
CHEMBL5091850 1 4.66
CHEMBL5092902 1 4.56
CHEMBL5090756 1 4.45
CHEMBL5081523 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087073 IC50 = 5.0 nM 8.30
CHEMBL4591082 SR-302 IC50 = 18.0 nM 7.75
CHEMBL5094236 IC50 = 1160.0 nM 5.94
CHEMBL5075462 IC50 = 1750.0 nM 5.76
CHEMBL5084386 IC50 = 2060.0 nM 5.69
CHEMBL5081039 IC50 = 3460.0 nM 5.46
CHEMBL5079394 IC50 = 3720.0 nM 5.43
CHEMBL4756586 IC50 = 4000.0 nM 5.40
CHEMBL4778587 IC50 = 5250.0 nM 5.28
CHEMBL5086352 IC50 = 7460.0 nM 5.13
CHEMBL4568183 SR-301 IC50 = 15500.0 nM 4.81
CHEMBL5092076 IC50 = 21500.0 nM 4.67
CHEMBL5091850 IC50 = 22000.0 nM 4.66
CHEMBL5092902 IC50 = 27700.0 nM 4.56
CHEMBL5090756 IC50 = 35200.0 nM 4.45
CHEMBL5081523 IC50 = 59200.0 nM 4.23