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Assay Detail

CHEMBL5738463

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Binding
Protein-Protein Interaction Assay: MCL-1/Noxa BH3 Peptide (MCL-1 Assay): The dose-dependent inhibition by the compounds described in this invention of the interaction between MCL-1 and the BH3 domain of Noxa (both human) was determined using a steady state binding competition assay with time-resolved fluorescence energy transfer (TR-FRET) readout. For that purpose MCL-1 (amino acids 173-321, N-terminal fused to Maltose Binding Protein (MBP) SEQ ID 1)) and a synthetic Noxa BH3-derived peptide of sequence Biotin-PEG2-PEG2-PAELEVE-Nva-ATQLRRFGDKLNFRQKLL-amide (SEQ ID 2) served as protein receptor and tracer ligand respectively. The MBP-MCL-1 was purchased from Beryllium (Bedford, Mass., USA). The expression and purification of this protein construct has been described elsewhere (DOI:10.1371/journal.pone.0125010). The Noxa BH3-derived peptide can be obtained from e.g. Biosyntan (Berlin, Germany).
ChEMBL ↗
321
Total Activities
35
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Substituted macrocyclic indole derivatives
(2022)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 107 8.51 9.59
kon 107 - -
k_off 107 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5832393 — — 9 9.59
CHEMBL5827427 — — 9 9.48
CHEMBL5889903 — — 6 9.43
CHEMBL5758636 — — 9 9.43
CHEMBL5860185 — — 9 9.41
CHEMBL5762188 — — 9 9.39
CHEMBL5807778 — — 9 9.38
CHEMBL5865078 — — 18 9.34
CHEMBL5800744 — — 15 9.34
CHEMBL5956315 — — 3 9.32
CHEMBL5757645 — — 9 9.32
CHEMBL6037958 — — 9 9.28
CHEMBL5773045 — — 9 9.27
CHEMBL5802940 — — 9 9.27
CHEMBL5846128 — — 9 9.24
CHEMBL6012019 — — 21 9.22
CHEMBL5799393 — — 9 9.20
CHEMBL5849709 — — 9 9.14
CHEMBL5860779 — — 9 9.14
CHEMBL5903890 — — 12 9.11
CHEMBL5752265 — — 18 9.10
CHEMBL5889625 — — 9 9.10
CHEMBL5760827 — — 12 9.06
CHEMBL5850731 — — 6 9.03
CHEMBL5946511 — — 9 9.00
CHEMBL5788230 — — 9 8.96
CHEMBL5998283 — — 6 8.96
CHEMBL5925747 — — 12 8.96
CHEMBL5950339 — — 9 8.92
CHEMBL5744208 — — 9 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5832393 — IC50 = 0.26 nM 9.59
CHEMBL5827427 — IC50 = 0.33 nM 9.48
CHEMBL5758636 — IC50 = 0.37 nM 9.43
CHEMBL5889903 — IC50 = 0.37 nM 9.43
CHEMBL5860185 — IC50 = 0.39 nM 9.41
CHEMBL5762188 — IC50 = 0.41 nM 9.39
CHEMBL5807778 — IC50 = 0.42 nM 9.38
CHEMBL5865078 — IC50 = 0.46 nM 9.34
CHEMBL5800744 — IC50 = 0.46 nM 9.34
CHEMBL5956315 — IC50 = 0.48 nM 9.32
CHEMBL5757645 — IC50 = 0.48 nM 9.32
CHEMBL6037958 — IC50 = 0.53 nM 9.28
CHEMBL5827427 — IC50 = 0.52 nM 9.28
CHEMBL5865078 — IC50 = 0.53 nM 9.28
CHEMBL5773045 — IC50 = 0.54 nM 9.27
CHEMBL5802940 — IC50 = 0.54 nM 9.27
CHEMBL5860185 — IC50 = 0.55 nM 9.26
CHEMBL5846128 — IC50 = 0.57 nM 9.24
CHEMBL6012019 — IC50 = 0.6 nM 9.22
CHEMBL5799393 — IC50 = 0.63 nM 9.20
CHEMBL6012019 — IC50 = 0.64 nM 9.19
CHEMBL5846128 — IC50 = 0.66 nM 9.18
CHEMBL5800744 — IC50 = 0.69 nM 9.16
CHEMBL5802940 — IC50 = 0.72 nM 9.14
CHEMBL5849709 — IC50 = 0.72 nM 9.14
CHEMBL5860779 — IC50 = 0.73 nM 9.14
CHEMBL5903890 — IC50 = 0.78 nM 9.11
CHEMBL5903890 — IC50 = 0.78 nM 9.11
CHEMBL5889625 — IC50 = 0.79 nM 9.10
CHEMBL5752265 — IC50 = 0.8 nM 9.10
CHEMBL5903890 — IC50 = 0.84 nM 9.08
CHEMBL5757645 — IC50 = 0.85 nM 9.07
CHEMBL5800744 — IC50 = 0.88 nM 9.06
CHEMBL5760827 — IC50 = 0.88 nM 9.06
CHEMBL5762188 — IC50 = 0.88 nM 9.06
CHEMBL5850731 — IC50 = 0.94 nM 9.03
CHEMBL6012019 — IC50 = 0.95 nM 9.02
CHEMBL5865078 — IC50 = 1.0 nM 9.00
CHEMBL5946511 — IC50 = 1.0 nM 9.00
CHEMBL5758636 — IC50 = 1.0 nM 9.00
CHEMBL5752265 — IC50 = 1.0 nM 9.00
CHEMBL5760827 — IC50 = 1.1 nM 8.96
CHEMBL5998283 — IC50 = 1.1 nM 8.96
CHEMBL5832393 — IC50 = 1.1 nM 8.96
CHEMBL5760827 — IC50 = 1.1 nM 8.96
CHEMBL5752265 — IC50 = 1.1 nM 8.96
CHEMBL6012019 — IC50 = 1.1 nM 8.96
CHEMBL5925747 — IC50 = 1.1 nM 8.96
CHEMBL5860779 — IC50 = 1.1 nM 8.96
CHEMBL5788230 — IC50 = 1.1 nM 8.96