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Assay Detail

CHEMBL4420663

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

Binding
Inhibition of human LATS1 kinase domain (589 to 1130 amino acids) incubated for 1 hr in presence of Fluo-SGKtide substrate by fluorescence detection based biochemical caliper assay
45
Total Activities
45
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

Serine/threonine-protein kinase LATS1 (CHEMBL6167)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-6 Fused Bicyclic Heteroaryl Compounds and their Use as LATS Inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.86 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4439972 1 9.15
CHEMBL4447153 1 9.10
CHEMBL4525078 1 9.10
CHEMBL4446217 1 8.92
CHEMBL4590309 1 8.92
CHEMBL4456826 1 8.74
CHEMBL4483764 1 8.72
CHEMBL4476463 1 8.64
CHEMBL3338837 1 8.62
CHEMBL4465820 1 8.52
CHEMBL4436919 1 8.51
CHEMBL4439805 1 8.43
CHEMBL4476521 1 8.42
CHEMBL2147535 1 8.42
CHEMBL4468766 1 8.35
CHEMBL4464441 1 8.35
CHEMBL4472021 1 8.30
CHEMBL4563473 1 8.28
CHEMBL4566594 1 8.21
CHEMBL4459788 1 8.12
CHEMBL4566901 1 8.12
CHEMBL4448408 1 8.02
CHEMBL4440342 1 8.00
CHEMBL4463799 1 7.99
CHEMBL4448628 1 7.98
CHEMBL4461790 1 7.98
CHEMBL4448179 1 7.80
CHEMBL4566717 1 7.72
CHEMBL4565212 1 7.54
CHEMBL4565547 1 7.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4439972 IC50 = 0.7 nM 9.15
CHEMBL4447153 IC50 = 0.8 nM 9.10
CHEMBL4525078 IC50 = 0.8 nM 9.10
CHEMBL4446217 IC50 = 1.2 nM 8.92
CHEMBL4590309 IC50 = 1.2 nM 8.92
CHEMBL4456826 IC50 = 1.8 nM 8.74
CHEMBL4483764 IC50 = 1.9 nM 8.72
CHEMBL4476463 IC50 = 2.3 nM 8.64
CHEMBL3338837 IC50 = 2.4 nM 8.62
CHEMBL4465820 IC50 = 3.0 nM 8.52
CHEMBL4436919 IC50 = 3.1 nM 8.51
CHEMBL4439805 IC50 = 3.7 nM 8.43
CHEMBL4476521 IC50 = 3.8 nM 8.42
CHEMBL2147535 IC50 = 3.8 nM 8.42
CHEMBL4464441 IC50 = 4.5 nM 8.35
CHEMBL4468766 IC50 = 4.5 nM 8.35
CHEMBL4472021 IC50 = 5.0 nM 8.30
CHEMBL4563473 IC50 = 5.2 nM 8.28
CHEMBL4566594 IC50 = 6.1 nM 8.21
CHEMBL4459788 IC50 = 7.6 nM 8.12
CHEMBL4566901 IC50 = 7.5 nM 8.12
CHEMBL4448408 IC50 = 9.6 nM 8.02
CHEMBL4440342 IC50 = 10.0 nM 8.00
CHEMBL4463799 IC50 = 10.2 nM 7.99
CHEMBL4448628 IC50 = 10.4 nM 7.98
CHEMBL4461790 IC50 = 10.5 nM 7.98
CHEMBL4448179 IC50 = 16.0 nM 7.80
CHEMBL4566717 IC50 = 18.9 nM 7.72
CHEMBL4565212 IC50 = 29.2 nM 7.54
CHEMBL4565547 IC50 = 42.5 nM 7.37
CHEMBL4461247 IC50 = 43.3 nM 7.36
CHEMBL4549171 IC50 = 58.1 nM 7.24
CHEMBL4457273 IC50 = 57.2 nM 7.24
CHEMBL4577411 IC50 = 59.0 nM 7.23
CHEMBL4522691 IC50 = 59.5 nM 7.22
CHEMBL4556611 IC50 = 68.7 nM 7.16
CHEMBL4464722 IC50 = 97.1 nM 7.01
CHEMBL4470844 IC50 = 125.1 nM 6.90
CHEMBL4444841 IC50 = 163.9 nM 6.79
CHEMBL4483670 IC50 = 208.9 nM 6.68
CHEMBL4438995 IC50 = 457.0 nM 6.34
CHEMBL4539019 IC50 = 466.7 nM 6.33
CHEMBL4551335 IC50 = 662.9 nM 6.18
CHEMBL4442656 IC50 = 1033.6 nM 5.99
CHEMBL4527014 IC50 - -