Linker Information
General Information of This Linker
| Linker ID |
LIN0ZTGLB
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| Linker Name |
H1H21234N-N297Q- LP2 lINKER
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C110H171N17O47
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| Isosmiles |
CC([C@H](NC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1C2=C(C=CC=C2)C3=C(N(N=N3)CCCCCOCCOCCN)C4=C(C1)C=CC=C4)=O)=O)=O)CCCCNC(COC5CCCCCC6=C5N=NN6CNC(COC7CCCCCC8=C7N=NN8C[C@@H]9O[C@@H](O[C@H]%10C(O)[C@H](O)[C@@H](O[C@H](O%11)[C@@H](O)[C@H](O)[C@@H](O[C@@H]%12[C@H](O)C(O)[C@H](O[C@@H](O%13)[C@H](O)[C@H](O)[C@H](O[C@@H]%14[C@H](O)C([C@H](O)[C@H](O%14)CO)O)[C@H]%13CO)[C@H](O%12)CO)[C@@H]%11CO)[C@@H](O%10)CO)[C@@H](O)C(O)C9O)=O)=O)=O)C(N[C@@H](C)C(O)=O)=O)C
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| InChI |
InChI=1S/C110H171N17O47/c1-57(2)79(103(153)115-58(3)104(154)155)117-102(152)62(116-75(134)30-36-157-40-43-160-45-46-161-44-42-159-38-33-113-74(133)28-29-78(137)124-47-59-19-11-12-20-60(59)83-80(61-21-13-14-23-63(61)124)118-121-125(83)34-17-6-18-35-156-39-41-158-37-31-111)22-15-16-32-112-76(135)54-162-67-27-10-5-8-25-65-82(67)120-123-127(65)56-114-77(136)55-163-66-26-9-4-7-24-64-81(66)119-122-126(64)48-68-84(138)86(140)93(147)109(164-68)174-110-97(151)91(145)101(73(53-132)169-110)173-108-96(150)90(144)100(72(52-131)168-108)172-107-95(149)89(143)99(71(51-130)167-107)171-106-94(148)88(142)98(70(50-129)166-106)170-105-92(146)87(141)85(139)69(49-128)165-105/h11-14,19-21,23,57-58,62,66-73,79,84-101,105-110,128-132,138-151H,4-10,15-18,22,24-56,111H2,1-3H3,(H,112,135)(H,113,133)(H,114,136)(H,115,153)(H,116,134)(H,117,152)(H,154,155)/t58-,62+,66?,67?,68-,69+,70+,71+,72-,73-,79-,84?,85+,86?,87?,88-,89?,90-,91-,92+,93-,94+,95+,96-,97?,98+,99+,100-,101-,105+,106+,107+,108-,109-,110-/m0/s1
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| InChIKey |
DFWKMVADXLCIHE-FZKQQEGFSA-N
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| Pharmaceutical Properties |
Molecule Weight
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2483.65
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Polar area
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910.1
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Complexity
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.
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xlogp Value
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-9.5984
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Heavy Count
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174
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Rot Bonds
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66
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Hbond acc
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56
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Hbond Donor
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27
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
H1H21234N-N297Q-LP2 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.868 nM
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Positive MSR1 expression (MSR1+++/++) | ||
| Method Description |
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-4/LXR-Luc cells
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP-1/LXR-Luc cells | CVCL_5115 | ||
References
