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Assay Detail

CHEMBL4052575

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

Binding
Inhibition of full length human C-terminal 6-His-tagged ATXbeta using FS-3 as substrate preincubated for 20 mins followed by substrate addition by fluorescence assay
25
Total Activities
25
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

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Repurposing Suzuki Coupling Reagents as a Directed Fragment Library Targeting Serine Hydrolases and Related Enzymes.
Lanier M, Cole DC, Istratiy Y, Klein MG, Schwartz PA, Tjhen R, Jennings A, Hixon MS.
J Med Chem (2017) 60 : 5209 -5215
PubMed 28564542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.86 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086456 1 6.50
CHEMBL4095509 1 6.30
CHEMBL4081848 1 6.00
CHEMBL4105287 1 5.80
CHEMBL4071778 1 5.70
CHEMBL1209679 1 5.50
CHEMBL348732 1 5.40
CHEMBL21427 1 5.30
CHEMBL4087433 1 5.30
CHEMBL500339 1 5.30
CHEMBL4084348 1 5.30
CHEMBL3218996 1 5.00
CHEMBL4082284 1 5.00
CHEMBL2146990 1 5.00
CHEMBL21485 PHENYLBORONIC ACID 1 5.00
CHEMBL349516 1 4.90
CHEMBL20852 1 4.90
CHEMBL485741 1 4.70
CHEMBL485740 1 4.70
CHEMBL4060380 1 3.70
CHEMBL4079823 1 3.60
CHEMBL275339 1 3.30
CHEMBL66861 1 3.20
CHEMBL1229732 1 3.10
CHEMBL4069065 1 2.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086456 IC50 = 316.23 nM 6.50
CHEMBL4095509 IC50 = 501.19 nM 6.30
CHEMBL4081848 IC50 = 1000.0 nM 6.00
CHEMBL4105287 IC50 = 1584.89 nM 5.80
CHEMBL4071778 IC50 = 1995.26 nM 5.70
CHEMBL1209679 IC50 = 3162.28 nM 5.50
CHEMBL348732 IC50 = 3981.07 nM 5.40
CHEMBL21427 IC50 = 5011.87 nM 5.30
CHEMBL4087433 IC50 = 5011.87 nM 5.30
CHEMBL500339 IC50 = 5011.87 nM 5.30
CHEMBL4084348 IC50 = 5011.87 nM 5.30
CHEMBL3218996 IC50 = 10000.0 nM 5.00
CHEMBL4082284 IC50 = 10000.0 nM 5.00
CHEMBL2146990 IC50 = 10000.0 nM 5.00
CHEMBL21485 PHENYLBORONIC ACID IC50 = 10000.0 nM 5.00
CHEMBL349516 IC50 = 12589.25 nM 4.90
CHEMBL20852 IC50 = 12589.25 nM 4.90
CHEMBL485741 IC50 = 19952.62 nM 4.70
CHEMBL485740 IC50 = 19952.62 nM 4.70
CHEMBL4060380 IC50 = 199526.23 nM 3.70
CHEMBL4079823 IC50 = 251188.64 nM 3.60
CHEMBL275339 IC50 = 501187.23 nM 3.30
CHEMBL66861 IC50 = 630957.34 nM 3.20
CHEMBL1229732 IC50 = 794328.23 nM 3.10
CHEMBL4069065 IC50 = 1258925.41 nM 2.90