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Assay Detail

CHEMBL4420664

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Binding
Inhibition of LATS in human HaCaT cells assessed as reduction in YAP phosphorylation level incubated for 2 hrs by HTRF assay
ChEMBL ↗
244
Total Activities
244
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase LATS (CHEMBL4523992) ↗
Type PROTEIN FAMILY
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 244 5.58 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4551441 — — 1 7.72
CHEMBL4472285 — — 1 7.72
CHEMBL4566869 — — 1 7.58
CHEMBL4577857 — — 1 7.40
CHEMBL4517252 — — 1 7.20
CHEMBL4531857 — — 1 7.17
CHEMBL4443335 — — 1 6.95
CHEMBL4472306 — — 1 6.88
CHEMBL4518582 — — 1 6.85
CHEMBL4471995 — — 1 6.78
CHEMBL4571192 — — 1 6.73
CHEMBL4573735 — — 1 6.73
CHEMBL4470612 — — 1 6.70
CHEMBL4454440 — — 1 6.70
CHEMBL4444109 — — 1 6.53
CHEMBL4576185 — — 1 6.48
CHEMBL4572019 — — 1 6.43
CHEMBL4513243 — — 1 6.42
CHEMBL4463150 — — 1 6.38
CHEMBL4585067 — — 1 6.38
CHEMBL4438081 — — 1 6.37
CHEMBL4520021 — — 1 6.32
CHEMBL4517907 — — 1 6.31
CHEMBL4532021 — — 1 6.27
CHEMBL4555291 — — 1 6.27
CHEMBL4439529 — — 1 6.26
CHEMBL4460905 — — 1 6.25
CHEMBL4446730 — — 1 6.22
CHEMBL4533967 — — 1 6.22
CHEMBL4453243 — — 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4472285 — IC50 = 19.0 nM 7.72
CHEMBL4551441 — IC50 = 19.0 nM 7.72
CHEMBL4566869 — IC50 = 26.0 nM 7.58
CHEMBL4577857 — IC50 = 40.0 nM 7.40
CHEMBL4517252 — IC50 = 63.0 nM 7.20
CHEMBL4531857 — IC50 = 67.0 nM 7.17
CHEMBL4443335 — IC50 = 113.0 nM 6.95
CHEMBL4472306 — IC50 = 131.0 nM 6.88
CHEMBL4518582 — IC50 = 141.0 nM 6.85
CHEMBL4471995 — IC50 = 165.0 nM 6.78
CHEMBL4571192 — IC50 = 185.0 nM 6.73
CHEMBL4573735 — IC50 = 187.0 nM 6.73
CHEMBL4454440 — IC50 = 202.0 nM 6.70
CHEMBL4470612 — IC50 = 198.0 nM 6.70
CHEMBL4444109 — IC50 = 294.0 nM 6.53
CHEMBL4576185 — IC50 = 330.0 nM 6.48
CHEMBL4572019 — IC50 = 370.0 nM 6.43
CHEMBL4513243 — IC50 = 380.0 nM 6.42
CHEMBL4463150 — IC50 = 422.0 nM 6.38
CHEMBL4585067 — IC50 = 414.0 nM 6.38
CHEMBL4438081 — IC50 = 423.0 nM 6.37
CHEMBL4520021 — IC50 = 476.0 nM 6.32
CHEMBL4517907 — IC50 = 488.0 nM 6.31
CHEMBL4532021 — IC50 = 534.0 nM 6.27
CHEMBL4555291 — IC50 = 539.0 nM 6.27
CHEMBL4439529 — IC50 = 550.0 nM 6.26
CHEMBL4460905 — IC50 = 565.0 nM 6.25
CHEMBL4446730 — IC50 = 606.0 nM 6.22
CHEMBL4453243 — IC50 = 606.0 nM 6.22
CHEMBL4533967 — IC50 = 607.0 nM 6.22
CHEMBL4436873 — IC50 = 646.0 nM 6.19
CHEMBL4465888 — IC50 = 660.0 nM 6.18
CHEMBL4554641 — IC50 = 656.0 nM 6.18
CHEMBL4446641 — IC50 = 765.0 nM 6.12
CHEMBL4463018 — IC50 = 765.0 nM 6.12
CHEMBL4520049 — IC50 = 782.0 nM 6.11
CHEMBL4472973 — IC50 = 853.0 nM 6.07
CHEMBL4547445 — IC50 = 895.0 nM 6.05
CHEMBL4564805 — IC50 = 977.0 nM 6.01
CHEMBL4592930 — IC50 = 1050.0 nM 5.98
CHEMBL4574721 — IC50 = 1150.0 nM 5.94
CHEMBL4563697 — IC50 = 1140.0 nM 5.94
CHEMBL4592699 — IC50 = 1150.0 nM 5.94
CHEMBL4578137 — IC50 = 1170.0 nM 5.93
CHEMBL4440182 — IC50 = 1210.0 nM 5.92
CHEMBL4437570 — IC50 = 1230.0 nM 5.91
CHEMBL4464251 — IC50 = 1240.0 nM 5.91
CHEMBL4470043 — IC50 = 1240.0 nM 5.91
CHEMBL4471884 — IC50 = 1430.0 nM 5.84
CHEMBL4562948 — IC50 = 1520.0 nM 5.82