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JNJ-4355

2D structure
Target MCL1 
Targeted domain BCL domain
Mode of action Inhibitor
Control JNJ-78732576
Recommended cellular usage concentration ≤ 10 µM
In vivo use Yes
Synonyms JNJ-78394355
Donated by Johnson & Johnson


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: Tb-MCL1: Ki = 0.015 nM (HTRF assay)
Selectivity within target family: > 30-fold HTRF assay: hBCL2 (Ki > 3.75 µM, closest related protein); hBCL2A1 (BFL-1) (Ki > 5 µM); hBCL2L1 (BCL-XL) (Ki > 5 µM)
Selectivity outside target family CEREP panel (76 targets) at 1 µM (% inhibition): Closest hits: glycine (strychnine-insensitive) = 16%; BZDp (TSPO ) (h) = 19,1 %; KATP channel = 11.21 %; Cl- channel (GABA-gated) = 22.6%; PTGS2(COX2) (h) = 20.2%, others < 10 % inhibition; PDSP screen (43 targets at 10 µM) clean except for OPRD1 (Ki = 870.56 nM)
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: Caspase Glo MOLP-8 assay: AC50 = 12 nM; Caspase Glo KMS12PE AC50 = 69 nM; Caspase Glo KMS12PE KO AC50 > 30 µM
Control compound (100 times less potent than the probe) JNJ-78732576: HTRF assay Ki = 115 nM (> 7000 times); Caspase Glo MOLP-8 assay: AC50 > 30 µM; Caspase Glo KMS12PE AC50 > 30 µM; Caspase Glo KMS12PE KO AC50 > 10 µM; Closest off-targets in the PDSP screen (43 targets at 10 µM) are HTR1A (Ki = 1698.16 nM), HTR5A (Ki = 2474.31 nM), SLC6A2 (Ki = 2882.07 nM), OPRD1 (Ki = 3226.28 nM).