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Assay Detail

CHEMBL3796495

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

Functional
Disruption of trabecular meshwork in human TM1 cells assessed as actin fiber length and focal adhesions by Hoechst staining based analysis
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type TM1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
Sturdivant JM, Royalty SM, Lin CW, Moore LA, Yingling JD, Laethem CL, Sherman B, Heintzelman GR, Kopczynski CC, deLong MA.
Bioorg Med Chem Lett (2016) 26 : 2475 -2480
PubMed 27072905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 6.65 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3793381 1 7.85
CHEMBL3794308 1 7.42
CHEMBL3792673 1 7.41
CHEMBL3793688 1 7.36
CHEMBL3793004 1 7.33
CHEMBL3793538 1 7.33
CHEMBL3792888 1 7.32
CHEMBL3793788 1 7.19
CHEMBL3794104 1 7.19
CHEMBL3792412 1 7.19
CHEMBL3793969 1 7.16
CHEMBL3792969 1 7.14
CHEMBL3792599 1 7.13
CHEMBL3794444 1 7.08
CHEMBL3793489 1 7.05
CHEMBL3792921 1 6.99
CHEMBL3793516 1 6.96
CHEMBL3793029 1 6.93
CHEMBL3770836 1 6.91
CHEMBL3794270 1 6.86
CHEMBL3792435 1 6.81
CHEMBL3794435 1 6.78
CHEMBL3792549 1 6.72
CHEMBL3793497 1 6.71
CHEMBL3792663 1 6.71
CHEMBL3792666 1 6.70
CHEMBL3793404 1 6.68
CHEMBL3793153 1 6.67
CHEMBL3792593 1 6.67
CHEMBL3792581 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3793381 IC50 = 14.0 nM 7.85
CHEMBL3794308 IC50 = 38.0 nM 7.42
CHEMBL3792673 IC50 = 39.0 nM 7.41
CHEMBL3793688 IC50 = 44.0 nM 7.36
CHEMBL3793004 IC50 = 47.0 nM 7.33
CHEMBL3793538 IC50 = 47.0 nM 7.33
CHEMBL3792888 IC50 = 48.0 nM 7.32
CHEMBL3793788 IC50 = 65.0 nM 7.19
CHEMBL3794104 IC50 = 64.0 nM 7.19
CHEMBL3792412 IC50 = 65.0 nM 7.19
CHEMBL3793969 IC50 = 70.0 nM 7.16
CHEMBL3792969 IC50 = 72.0 nM 7.14
CHEMBL3792599 IC50 = 74.0 nM 7.13
CHEMBL3794444 IC50 = 83.0 nM 7.08
CHEMBL3793489 IC50 = 90.0 nM 7.05
CHEMBL3792921 IC50 = 102.0 nM 6.99
CHEMBL3793516 IC50 = 111.0 nM 6.96
CHEMBL3793029 IC50 = 118.0 nM 6.93
CHEMBL3770836 IC50 = 123.0 nM 6.91
CHEMBL3794270 IC50 = 139.0 nM 6.86
CHEMBL3792435 IC50 = 156.0 nM 6.81
CHEMBL3794435 IC50 = 167.0 nM 6.78
CHEMBL3792549 IC50 = 192.0 nM 6.72
CHEMBL3793497 IC50 = 193.0 nM 6.71
CHEMBL3792663 IC50 = 193.0 nM 6.71
CHEMBL3792666 IC50 = 201.0 nM 6.70
CHEMBL3793404 IC50 = 208.0 nM 6.68
CHEMBL3793153 IC50 = 214.0 nM 6.67
CHEMBL3792593 IC50 = 214.0 nM 6.67
CHEMBL3792581 IC50 = 219.0 nM 6.66
CHEMBL3792689 IC50 = 248.0 nM 6.61
CHEMBL3794389 IC50 = 250.0 nM 6.60
CHEMBL3792781 IC50 = 266.0 nM 6.58
CHEMBL3794409 IC50 = 278.0 nM 6.56
CHEMBL3793203 IC50 = 298.0 nM 6.53
CHEMBL3794198 IC50 = 324.0 nM 6.49
CHEMBL3793659 IC50 = 330.0 nM 6.48
CHEMBL3793505 IC50 = 383.0 nM 6.42
CHEMBL3793243 IC50 = 424.0 nM 6.37
CHEMBL3793235 IC50 = 493.0 nM 6.31
CHEMBL3794298 IC50 = 672.0 nM 6.17
CHEMBL3792612 IC50 = 832.0 nM 6.08
CHEMBL3793245 IC50 = 1216.0 nM 5.92
CHEMBL3793870 IC50 = 1250.0 nM 5.90
CHEMBL3792734 IC50 = 1721.0 nM 5.76
CHEMBL3792603 IC50 = 2459.0 nM 5.61
CHEMBL3793296 IC50 = 4239.0 nM 5.37
CHEMBL3793368 IC50 = 4239.0 nM 5.37
CHEMBL3770730 IC50 = 5609.0 nM 5.25
CHEMBL3794254 IC50 = 11002.0 nM 4.96