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Assay Detail

CHEMBL4625187

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

Binding
Inhibition of collagenase (unknown origin) transfected in human HeLa cells by luciferase reporter gene assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of the potent non-steroidal glucocorticoid receptor modulator BAY 1003803 as clinical candidate.
Berger M, May E, Rehwinkel H, Schäcke H, Neuhaus R, Rottmann A, Zollner TM, Jaroch S.
Bioorg Med Chem Lett (2020) 30 : 127298 -127298
PubMed 32631518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.48 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4649732 1 9.60
CHEMBL4636181 1 9.40
CHEMBL3893393 1 9.20
CHEMBL4638643 1 9.10
CHEMBL4648762 1 9.00
CHEMBL4648597 1 8.90
CHEMBL4647176 1 8.80
CHEMBL4638451 1 8.80
CHEMBL4647195 1 8.80
CHEMBL4637784 1 8.50
CHEMBL4641137 1 8.40
CHEMBL4637332 1 8.30
CHEMBL4641422 1 8.20
CHEMBL384467 DEXAMETHASONE 4.0 1 8.10
CHEMBL4633027 1 8.00
CHEMBL4637564 1 8.00
CHEMBL4633793 1 8.00
CHEMBL4641098 1 8.00
CHEMBL4644529 1 7.90
CHEMBL4641316 1 7.60
CHEMBL4641277 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4649732 EC50 = 0.2512 nM 9.60
CHEMBL4636181 EC50 = 0.3981 nM 9.40
CHEMBL3893393 EC50 = 0.631 nM 9.20
CHEMBL4638643 EC50 = 0.7943 nM 9.10
CHEMBL4648762 EC50 = 1.0 nM 9.00
CHEMBL4648597 EC50 = 1.259 nM 8.90
CHEMBL4647176 EC50 = 1.585 nM 8.80
CHEMBL4638451 EC50 = 1.585 nM 8.80
CHEMBL4647195 EC50 = 1.585 nM 8.80
CHEMBL4637784 EC50 = 3.162 nM 8.50
CHEMBL4641137 EC50 = 3.981 nM 8.40
CHEMBL4637332 EC50 = 5.012 nM 8.30
CHEMBL4641422 EC50 = 6.31 nM 8.20
CHEMBL384467 DEXAMETHASONE EC50 = 7.943 nM 8.10
CHEMBL4633027 EC50 = 10.0 nM 8.00
CHEMBL4637564 EC50 = 10.0 nM 8.00
CHEMBL4633793 EC50 = 10.0 nM 8.00
CHEMBL4641098 EC50 = 10.0 nM 8.00
CHEMBL4644529 EC50 = 12.59 nM 7.90
CHEMBL4641316 EC50 = 25.12 nM 7.60
CHEMBL4641277 EC50 = 39.81 nM 7.40