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Assay Detail

CHEMBL4328666

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Binding
Inhibition of human GST-tagged catalytic ROCK1 expressed in baculovirus system using STK S2 peptide substrate and and 33P-ATP after 60 mins by HTRF assay
ChEMBL ↗
44
Total Activities
44
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

Rho-associated protein kinase 1 (CHEMBL3231) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design.
Hobson AD, Judge RA, Aguirre AL, Brown BS, Cui Y, Ding P, Dominguez E, DiGiammarino E, Egan DA, Freiberg GM, Gopalakrishnan SM, Harris CM, Honore MP, Kage KL, Kapecki NJ, Ling C, Ma J, Mack H, Mamo M, Maurus S, McRae B, Moore NS, Mueller BK, Mueller R, Namovic MT, Patel K, Pratt SD, Putman CB, Queeney KL, Sarris KK, Schaffter LM, Stoll V, Vasudevan A, Wang L, Wang L, Wirthl W, Yach K.
J Med Chem (2018) 61 : 11074 -11100
PubMed 30384606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 6.50 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4434688 — — 1 8.52
CHEMBL4472858 — — 1 7.96
CHEMBL4583341 — — 1 7.85
CHEMBL4448806 — — 1 7.77
CHEMBL4536833 — — 1 7.72
CHEMBL4469316 — — 1 7.41
CHEMBL4459077 — — 1 7.34
CHEMBL4459800 — — 1 7.07
CHEMBL4553926 — — 1 7.02
CHEMBL4474946 — — 1 6.96
CHEMBL4465725 — — 1 6.92
CHEMBL4436197 — — 1 6.86
CHEMBL2006299 — — 1 6.80
CHEMBL4557041 — — 1 6.80
CHEMBL4469434 — — 1 6.80
CHEMBL4572198 — — 1 6.72
CHEMBL4460511 — — 1 6.68
CHEMBL4521871 — — 1 6.62
CHEMBL4522042 — — 1 6.55
CHEMBL4463301 — — 1 6.55
CHEMBL4555093 — — 1 6.51
CHEMBL4436040 — — 1 6.47
CHEMBL4556370 — — 1 6.40
CHEMBL4476761 — — 1 6.28
CHEMBL1977135 — — 1 6.26
CHEMBL4471862 — — 1 6.26
CHEMBL4588929 — — 1 6.24
CHEMBL4438453 — — 1 6.21
CHEMBL4445356 — — 1 6.19
CHEMBL4451899 — — 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4434688 — IC50 = 3.0 nM 8.52
CHEMBL4472858 — IC50 = 11.0 nM 7.96
CHEMBL4583341 — IC50 = 14.0 nM 7.85
CHEMBL4448806 — IC50 = 17.0 nM 7.77
CHEMBL4536833 — IC50 = 19.0 nM 7.72
CHEMBL4469316 — IC50 = 39.0 nM 7.41
CHEMBL4459077 — IC50 = 46.0 nM 7.34
CHEMBL4459800 — IC50 = 85.0 nM 7.07
CHEMBL4553926 — IC50 = 95.0 nM 7.02
CHEMBL4474946 — IC50 = 110.0 nM 6.96
CHEMBL4465725 — IC50 = 120.0 nM 6.92
CHEMBL4436197 — IC50 = 139.0 nM 6.86
CHEMBL2006299 — IC50 = 160.0 nM 6.80
CHEMBL4469434 — IC50 = 160.0 nM 6.80
CHEMBL4557041 — IC50 = 160.0 nM 6.80
CHEMBL4572198 — IC50 = 190.0 nM 6.72
CHEMBL4460511 — IC50 = 210.0 nM 6.68
CHEMBL4521871 — IC50 = 240.0 nM 6.62
CHEMBL4522042 — IC50 = 280.0 nM 6.55
CHEMBL4463301 — IC50 = 280.0 nM 6.55
CHEMBL4555093 — IC50 = 310.0 nM 6.51
CHEMBL4436040 — IC50 = 340.0 nM 6.47
CHEMBL4556370 — IC50 = 400.0 nM 6.40
CHEMBL4476761 — IC50 = 520.0 nM 6.28
CHEMBL1977135 — IC50 = 550.0 nM 6.26
CHEMBL4471862 — IC50 = 550.0 nM 6.26
CHEMBL4588929 — IC50 = 580.0 nM 6.24
CHEMBL4438453 — IC50 = 610.0 nM 6.21
CHEMBL4445356 — IC50 = 650.0 nM 6.19
CHEMBL4451899 — IC50 = 720.0 nM 6.14
CHEMBL4577208 — IC50 = 720.0 nM 6.14
CHEMBL4454552 — IC50 = 780.0 nM 6.11
CHEMBL4570150 — IC50 = 1000.0 nM 6.00
CHEMBL4585481 — IC50 = 990.0 nM 6.00
CHEMBL4446212 — IC50 = 1500.0 nM 5.82
CHEMBL4590232 — IC50 = 1600.0 nM 5.80
CHEMBL4547725 — IC50 = 1700.0 nM 5.77
CHEMBL4550282 — IC50 = 1900.0 nM 5.72
CHEMBL4568447 — IC50 = 2400.0 nM 5.62
CHEMBL4475535 — IC50 = 4400.0 nM 5.36
CHEMBL4575880 — IC50 = 5100.0 nM 5.29
CHEMBL4584824 — IC50 = 9400.0 nM 5.03
CHEMBL4447521 — IC50 = 16000.0 nM 4.80
CHEMBL4540054 — IC50 > 10000.0 nM -