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Assay Detail

CHEMBL4845000

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

Binding
Binding affinity to human TIM-3 IgV domain (residues 22 to 130) expressed in Escherichia coli BL21 (DE3) by 1H-15N SOFAST-HMQC spectroscopic analysis
24
Total Activities
24
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

Hepatitis A virus cellular receptor 2 (CHEMBL4630879)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fragment-Based Discovery of Small Molecules Bound to T-Cell Immunoglobulin and Mucin Domain-Containing Molecule 3 (TIM-3).
Rietz TA, Teuscher KB, Mills JJ, Gogliotti RD, Lepovitz LT, Scaggs WR, Yoshida K, Luong K, Lee T, Fesik SW.
J Med Chem (2021) 64 : 14757 -14772
PubMed 34597046 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 24 3.94 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873902 1 6.60
CHEMBL4848599 1 5.70
CHEMBL4863477 1 5.00
CHEMBL4860123 1 4.40
CHEMBL4870128 1 4.40
CHEMBL4870200 1 4.40
CHEMBL4854696 1 4.40
CHEMBL4852144 1 4.30
CHEMBL4864057 1 4.05
CHEMBL4871549 1 4.05
CHEMBL4865760 1 3.89
CHEMBL4866110 1 3.60
CHEMBL4876694 1 3.48
CHEMBL4876887 1 3.35
CHEMBL1610810 1 3.34
CHEMBL1462057 1 3.28
CHEMBL69086 1 3.17
CHEMBL4854485 1 3.13
CHEMBL4864031 1 3.11
CHEMBL1569082 1 3.09
CHEMBL1576751 1 3.07
CHEMBL2132792 1 2.85
CHEMBL4867105 1 -
CHEMBL330116 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873902 Kd = 250.0 nM 6.60
CHEMBL4848599 Kd = 2000.0 nM 5.70
CHEMBL4863477 Kd = 10000.0 nM 5.00
CHEMBL4860123 Kd = 40000.0 nM 4.40
CHEMBL4870128 Kd = 40000.0 nM 4.40
CHEMBL4870200 Kd = 40000.0 nM 4.40
CHEMBL4854696 Kd = 40000.0 nM 4.40
CHEMBL4852144 Kd = 50000.0 nM 4.30
CHEMBL4864057 Kd = 90000.0 nM 4.05
CHEMBL4871549 Kd = 90000.0 nM 4.05
CHEMBL4865760 Kd = 130000.0 nM 3.89
CHEMBL4866110 Kd = 250000.0 nM 3.60
CHEMBL4876694 Kd = 330000.0 nM 3.48
CHEMBL4876887 Kd = 450000.0 nM 3.35
CHEMBL1610810 Kd = 460000.0 nM 3.34
CHEMBL1462057 Kd = 530000.0 nM 3.28
CHEMBL69086 Kd = 670000.0 nM 3.17
CHEMBL4854485 Kd = 740000.0 nM 3.13
CHEMBL4864031 Kd = 780000.0 nM 3.11
CHEMBL1569082 Kd = 810000.0 nM 3.09
CHEMBL1576751 Kd = 850000.0 nM 3.07
CHEMBL2132792 Kd = 1400000.0 nM 2.85
CHEMBL4867105 Kd > 2000000.0 nM -
CHEMBL330116 Kd > 2000000.0 nM -