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Assay Detail

CHEMBL5739337

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

Binding
Enzyme-linked immunosorbent assay (ELISA): Enzyme reaction substrate Poly(Glu, Tyr) 4:1 was diluted to 20 μg/mL with potassium-free PBS (10 mM sodium phosphate buffer, 150 mM NaCl, pH 7.2-7.4), and the microtiter plate was coated with 125 μL/well and placed at 37° C. for 12-16 hours of reaction. The liquid in the well was discard. The plate was washed three times with T-PBS (potassium-free PBS containing 0.1% Tween-20, 200 μL/well), 5 minutes each time. The ELISA plate was dried in an oven at 37° C. for 1 to 2 hours.
ChEMBL ↗
96
Total Activities
32
Compounds Tested
3
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

Fused ring pyrimidine amino compound and preparation method, pharmaceutical composition, and use thereof
(2023)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 8.83 11.00
kon 32 - -
k_off 32 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5938192 — — 3 11.00
CHEMBL5787536 — — 3 10.00
CHEMBL5781115 — — 3 10.00
CHEMBL5965095 — — 3 10.00
CHEMBL5756960 — — 3 9.70
CHEMBL5885968 — — 3 9.70
CHEMBL6051298 — — 3 9.70
CHEMBL6055194 — — 3 9.52
CHEMBL6027087 — — 3 9.52
CHEMBL6052146 — — 3 9.52
CHEMBL5758698 — — 3 9.40
CHEMBL6044993 — — 3 9.40
CHEMBL5829475 — — 3 9.30
CHEMBL5518031 — — 3 9.30
CHEMBL5848200 — — 3 9.22
CHEMBL5986782 — — 3 9.15
CHEMBL5974437 — — 3 9.10
CHEMBL5906159 — — 3 9.00
CHEMBL5900841 — — 3 8.96
CHEMBL5931136 — — 3 8.68
CHEMBL5752611 — — 3 8.64
CHEMBL5752161 — — 3 8.55
CHEMBL5822317 — — 3 8.48
CHEMBL6049180 — — 3 8.41
CHEMBL5886620 — — 3 8.24
CHEMBL5883823 — — 3 8.14
CHEMBL6015947 — — 3 7.00
CHEMBL6031079 — — 3 7.00
CHEMBL6028677 — — 3 7.00
CHEMBL5810160 — — 3 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5938192 — IC50 = 0.01 nM 11.00
CHEMBL5787536 — IC50 = 0.1 nM 10.00
CHEMBL5781115 — IC50 = 0.1 nM 10.00
CHEMBL5965095 — IC50 = 0.1 nM 10.00
CHEMBL5756960 — IC50 = 0.2 nM 9.70
CHEMBL6051298 — IC50 = 0.2 nM 9.70
CHEMBL5885968 — IC50 = 0.2 nM 9.70
CHEMBL6052146 — IC50 = 0.3 nM 9.52
CHEMBL6027087 — IC50 = 0.3 nM 9.52
CHEMBL6055194 — IC50 = 0.3 nM 9.52
CHEMBL5758698 — IC50 = 0.4 nM 9.40
CHEMBL6044993 — IC50 = 0.4 nM 9.40
CHEMBL5829475 — IC50 = 0.5 nM 9.30
CHEMBL5518031 — IC50 = 0.5 nM 9.30
CHEMBL5848200 — IC50 = 0.6 nM 9.22
CHEMBL5986782 — IC50 = 0.7 nM 9.15
CHEMBL5974437 — IC50 = 0.8 nM 9.10
CHEMBL5906159 — IC50 = 1.0 nM 9.00
CHEMBL5900841 — IC50 = 1.1 nM 8.96
CHEMBL5931136 — IC50 = 2.1 nM 8.68
CHEMBL5752611 — IC50 = 2.3 nM 8.64
CHEMBL5752161 — IC50 = 2.8 nM 8.55
CHEMBL5822317 — IC50 = 3.3 nM 8.48
CHEMBL6049180 — IC50 = 3.9 nM 8.41
CHEMBL5886620 — IC50 = 5.8 nM 8.24
CHEMBL5883823 — IC50 = 7.2 nM 8.14
CHEMBL6028677 — IC50 = 100.0 nM 7.00
CHEMBL6015947 — IC50 = 100.0 nM 7.00
CHEMBL5810160 — IC50 = 100.0 nM 7.00
CHEMBL6031079 — IC50 = 100.0 nM 7.00
CHEMBL6041106 — IC50 = 100.0 nM 7.00
CHEMBL5924215 — IC50 = 108.0 nM 6.97
CHEMBL5938192 — k_off = - s-1 -
CHEMBL5883823 — k_off = - s-1 -
CHEMBL5752611 — kon = - — -
CHEMBL5924215 — kon = - — -
CHEMBL5752611 — k_off = - s-1 -
CHEMBL6028677 — k_off = - s-1 -
CHEMBL5900841 — k_off = - s-1 -
CHEMBL5900841 — kon = - — -
CHEMBL6031079 — kon = - — -
CHEMBL6027087 — k_off = - s-1 -
CHEMBL6028677 — kon = - — -
CHEMBL6027087 — kon = - — -
CHEMBL6031079 — k_off = - s-1 -
CHEMBL6041106 — kon = - — -
CHEMBL6052146 — k_off = - s-1 -
CHEMBL6052146 — kon = - — -
CHEMBL6041106 — k_off = - s-1 -
CHEMBL5883823 — kon = - — -