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Assay Detail

CHEMBL3382270

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

Binding
Inhibition of human factor 10a using N-Z-D-Arg-Gly-Arg-pNA, S-2765 chromogenic substrate
ChEMBL ↗
54
Total Activities
54
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

Coagulation factor X (CHEMBL244) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.
Xue T, Ding S, Guo B, Zhou Y, Sun P, Wang H, Chu W, Gong G, Wang Y, Chen X, Yang Y.
J Med Chem (2014) 57 : 7770 -7791
PubMed 25179681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 6.63 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330482 — — 1 8.60
CHEMBL3330442 — — 1 8.47
CHEMBL3330490 — — 1 8.33
CHEMBL3330483 — — 1 8.31
CHEMBL3330493 — — 1 8.30
CHEMBL3330491 — — 1 8.18
CHEMBL198362 RIVAROXABAN 4.0 1 8.07
CHEMBL3330494 — — 1 7.82
CHEMBL3330486 — — 1 7.76
CHEMBL3330444 — — 1 7.69
CHEMBL3330488 — — 1 7.68
CHEMBL3330476 — — 1 7.49
CHEMBL3330461 — — 1 7.42
CHEMBL3330453 — — 1 7.39
CHEMBL3330484 — — 1 7.34
CHEMBL3330451 — — 1 7.33
CHEMBL3330487 — — 1 7.30
CHEMBL3330443 — — 1 7.24
CHEMBL3330462 — — 1 7.22
CHEMBL3330485 — — 1 7.19
CHEMBL3330458 — — 1 7.13
CHEMBL3330445 — — 1 7.06
CHEMBL3330475 — — 1 7.05
CHEMBL3330450 — — 1 6.89
CHEMBL3330463 — — 1 6.80
CHEMBL3330454 — — 1 6.72
CHEMBL3330479 — — 1 6.51
CHEMBL3330477 — — 1 6.25
CHEMBL3330448 — — 1 6.23
CHEMBL3330464 — — 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330482 — IC50 = 2.51 nM 8.60
CHEMBL3330442 — IC50 = 3.41 nM 8.47
CHEMBL3330490 — IC50 = 4.71 nM 8.33
CHEMBL3330483 — IC50 = 4.89 nM 8.31
CHEMBL3330493 — IC50 = 5.06 nM 8.30
CHEMBL3330491 — IC50 = 6.59 nM 8.18
CHEMBL198362 RIVAROXABAN IC50 = 8.52 nM 8.07
CHEMBL3330494 — IC50 = 15.2 nM 7.82
CHEMBL3330486 — IC50 = 17.37 nM 7.76
CHEMBL3330444 — IC50 = 20.22 nM 7.69
CHEMBL3330488 — IC50 = 20.87 nM 7.68
CHEMBL3330476 — IC50 = 32.08 nM 7.49
CHEMBL3330461 — IC50 = 37.65 nM 7.42
CHEMBL3330453 — IC50 = 40.56 nM 7.39
CHEMBL3330484 — IC50 = 45.22 nM 7.34
CHEMBL3330451 — IC50 = 46.64 nM 7.33
CHEMBL3330487 — IC50 = 50.52 nM 7.30
CHEMBL3330443 — IC50 = 57.81 nM 7.24
CHEMBL3330462 — IC50 = 60.56 nM 7.22
CHEMBL3330485 — IC50 = 63.96 nM 7.19
CHEMBL3330458 — IC50 = 74.77 nM 7.13
CHEMBL3330445 — IC50 = 87.17 nM 7.06
CHEMBL3330475 — IC50 = 88.53 nM 7.05
CHEMBL3330450 — IC50 = 130.0 nM 6.89
CHEMBL3330463 — IC50 = 160.0 nM 6.80
CHEMBL3330454 — IC50 = 190.0 nM 6.72
CHEMBL3330479 — IC50 = 310.0 nM 6.51
CHEMBL3330477 — IC50 = 560.0 nM 6.25
CHEMBL3330448 — IC50 = 590.0 nM 6.23
CHEMBL3330464 — IC50 = 710.0 nM 6.15
CHEMBL3330446 — IC50 = 730.0 nM 6.14
CHEMBL3330478 — IC50 = 1210.0 nM 5.92
CHEMBL3330452 — IC50 = 1220.0 nM 5.91
CHEMBL3330489 — IC50 = 1610.0 nM 5.79
CHEMBL3330469 — IC50 = 1750.0 nM 5.76
CHEMBL3330449 — IC50 = 1860.0 nM 5.73
CHEMBL3330455 — IC50 = 2210.0 nM 5.66
CHEMBL3330447 — IC50 = 2510.0 nM 5.60
CHEMBL3330459 — IC50 = 4180.0 nM 5.38
CHEMBL3330465 — IC50 = 4780.0 nM 5.32
CHEMBL3330460 — IC50 = 5530.0 nM 5.26
CHEMBL3330467 — IC50 = 7060.0 nM 5.15
CHEMBL3330466 — IC50 = 8080.0 nM 5.09
CHEMBL3330492 — IC50 = 8180.0 nM 5.09
CHEMBL3330457 — IC50 = 11360.0 nM 4.95
CHEMBL3330456 — IC50 = 15770.0 nM 4.80
CHEMBL3330470 — IC50 = 25880.0 nM 4.59
CHEMBL3330474 — IC50 = 52690.0 nM 4.28
CHEMBL3330481 — IC50 > 100000.0 nM -
CHEMBL3330480 — IC50 > 100000.0 nM -