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Assay Detail

CHEMBL915970

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Binding
Inhibition of Rho kinase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Rho-associated protein kinase (CHEMBL2111459)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design and synthesis of rho kinase inhibitors (III).
Iwakubo M, Takami A, Okada Y, Kawata T, Tagami Y, Sato M, Sugiyama T, Fukushima K, Taya S, Amano M, Kaibuchi K, Iijima H.
Bioorg Med Chem (2007) 15 : 1022 -1033
PubMed 17084087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.78 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387625 1 7.60
CHEMBL375556 1 7.19
CHEMBL223815 1 7.19
CHEMBL224361 1 7.16
CHEMBL387954 1 7.12
CHEMBL223336 1 7.02
CHEMBL389926 1 7.00
CHEMBL224505 1 6.85
CHEMBL266512 1 6.75
CHEMBL224360 1 6.75
CHEMBL38380 FASUDIL 3.0 1 6.75
CHEMBL225492 1 6.73
CHEMBL375735 1 6.71
CHEMBL388285 1 6.69
CHEMBL224508 1 6.68
CHEMBL375882 1 6.68
CHEMBL223907 1 6.63
CHEMBL389254 1 6.58
CHEMBL375736 1 6.57
CHEMBL373759 1 6.56
CHEMBL438783 1 6.51
CHEMBL224472 1 6.46
CHEMBL224362 1 6.36
CHEMBL224417 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387625 IC50 = 25.0 nM 7.60
CHEMBL375556 IC50 = 65.0 nM 7.19
CHEMBL223815 IC50 = 65.0 nM 7.19
CHEMBL224361 IC50 = 70.0 nM 7.16
CHEMBL387954 IC50 = 75.0 nM 7.12
CHEMBL223336 IC50 = 95.0 nM 7.02
CHEMBL389926 IC50 = 100.0 nM 7.00
CHEMBL224505 IC50 = 140.0 nM 6.85
CHEMBL266512 IC50 = 180.0 nM 6.75
CHEMBL224360 IC50 = 180.0 nM 6.75
CHEMBL38380 FASUDIL IC50 = 180.0 nM 6.75
CHEMBL225492 IC50 = 185.0 nM 6.73
CHEMBL375735 IC50 = 195.0 nM 6.71
CHEMBL388285 IC50 = 205.0 nM 6.69
CHEMBL224508 IC50 = 210.0 nM 6.68
CHEMBL375882 IC50 = 210.0 nM 6.68
CHEMBL223907 IC50 = 235.0 nM 6.63
CHEMBL389254 IC50 = 265.0 nM 6.58
CHEMBL375736 IC50 = 270.0 nM 6.57
CHEMBL373759 IC50 = 275.0 nM 6.56
CHEMBL438783 IC50 = 310.0 nM 6.51
CHEMBL224472 IC50 = 345.0 nM 6.46
CHEMBL224362 IC50 = 440.0 nM 6.36
CHEMBL224417 IC50 = 580.0 nM 6.24