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Assay Detail

CHEMBL4616526

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Binding
Inhibition of human ATX pre-incubated for 45 mins before fluorogenic substrate-3 addition and measured every minute for 30 mins by fluorescence based assay
ChEMBL ↗
53
Total Activities
53
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

Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great In Vivo Efficacy in a Mouse Lung Fibrosis Model.
Lei H, Guo M, Li X, Jia F, Li C, Yang Y, Cao M, Jiang N, Ma E, Zhai X.
J Med Chem (2020) 63 : 7326 -7346
PubMed 32479084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 6.64 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4640012 — — 1 9.37
CHEMBL4647222 — — 1 9.00
CHEMBL3828074 ZIRITAXESTAT 3.0 1 8.89
CHEMBL3186509 — — 1 8.57
CHEMBL4644036 — — 1 7.80
CHEMBL4641011 — — 1 7.67
CHEMBL4639039 — — 1 7.51
CHEMBL4643433 — — 1 7.47
CHEMBL4633587 — — 1 7.46
CHEMBL4643937 — — 1 7.43
CHEMBL4644515 — — 1 7.20
CHEMBL4634620 — — 1 7.16
CHEMBL4638125 — — 1 6.97
CHEMBL4644727 — — 1 6.93
CHEMBL4636755 — — 1 6.91
CHEMBL4638854 — — 1 6.90
CHEMBL4637219 — — 1 6.89
CHEMBL4636225 — — 1 6.87
CHEMBL4639826 — — 1 6.75
CHEMBL4634766 — — 1 6.70
CHEMBL4643457 — — 1 6.68
CHEMBL4643989 — — 1 6.64
CHEMBL4642973 — — 1 6.53
CHEMBL4646372 — — 1 6.29
CHEMBL4637140 — — 1 6.21
CHEMBL4635930 — — 1 6.21
CHEMBL4640212 — — 1 6.18
CHEMBL4636797 — — 1 6.13
CHEMBL4645651 — — 1 6.12
CHEMBL4647615 — — 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4640012 — IC50 = 0.43 nM 9.37
CHEMBL4647222 — IC50 = 1.01 nM 9.00
CHEMBL3828074 ZIRITAXESTAT IC50 = 1.3 nM 8.89
CHEMBL3186509 — IC50 = 2.7 nM 8.57
CHEMBL4644036 — IC50 = 15.7 nM 7.80
CHEMBL4641011 — IC50 = 21.3 nM 7.67
CHEMBL4639039 — IC50 = 30.7 nM 7.51
CHEMBL4643433 — IC50 = 34.1 nM 7.47
CHEMBL4633587 — IC50 = 34.7 nM 7.46
CHEMBL4643937 — IC50 = 36.9 nM 7.43
CHEMBL4644515 — IC50 = 62.7 nM 7.20
CHEMBL4634620 — IC50 = 69.4 nM 7.16
CHEMBL4638125 — IC50 = 107.4 nM 6.97
CHEMBL4644727 — IC50 = 117.0 nM 6.93
CHEMBL4636755 — IC50 = 121.8 nM 6.91
CHEMBL4638854 — IC50 = 127.0 nM 6.90
CHEMBL4637219 — IC50 = 127.3 nM 6.89
CHEMBL4636225 — IC50 = 134.9 nM 6.87
CHEMBL4639826 — IC50 = 180.0 nM 6.75
CHEMBL4634766 — IC50 = 199.4 nM 6.70
CHEMBL4643457 — IC50 = 210.0 nM 6.68
CHEMBL4643989 — IC50 = 231.1 nM 6.64
CHEMBL4642973 — IC50 = 297.2 nM 6.53
CHEMBL4646372 — IC50 = 507.9 nM 6.29
CHEMBL4635930 — IC50 = 613.0 nM 6.21
CHEMBL4637140 — IC50 = 610.0 nM 6.21
CHEMBL4640212 — IC50 = 655.0 nM 6.18
CHEMBL4636797 — IC50 = 740.0 nM 6.13
CHEMBL4645651 — IC50 = 757.0 nM 6.12
CHEMBL4647615 — IC50 = 879.0 nM 6.06
CHEMBL4643078 — IC50 = 906.0 nM 6.04
CHEMBL4641104 — IC50 = 970.0 nM 6.01
CHEMBL4644717 — IC50 = 1170.0 nM 5.93
CHEMBL4636002 — IC50 = 1320.0 nM 5.88
CHEMBL4635487 — IC50 = 1349.0 nM 5.87
CHEMBL4648648 — IC50 = 1370.0 nM 5.86
CHEMBL4649805 — IC50 = 1460.0 nM 5.84
CHEMBL4641845 — IC50 = 1550.0 nM 5.81
CHEMBL4636052 — IC50 = 1590.0 nM 5.80
CHEMBL4635805 — IC50 = 1840.0 nM 5.74
CHEMBL4644862 — IC50 = 2310.0 nM 5.64
CHEMBL4637835 — IC50 = 2530.0 nM 5.60
CHEMBL4645284 — IC50 = 2740.0 nM 5.56
CHEMBL4634132 — IC50 = 2870.0 nM 5.54
CHEMBL4634398 — IC50 = 3960.0 nM 5.40
CHEMBL4642425 — IC50 = 5240.0 nM 5.28
CHEMBL4633282 — IC50 > 10000.0 nM -
CHEMBL4642687 — IC50 > 10000.0 nM -
CHEMBL4640227 — IC50 > 10000.0 nM -
CHEMBL4646623 — IC50 > 10000.0 nM -